The immune system has evolved to survey and respond appropriately to the universe of foreign pathogens, deploying an intricate repertoire of mechanisms that keep responses to host tissues in check. The immune system is typically divided into two categories--innate and adaptive. Innate immunity refers to nonspecific defense mechanisms that come into play immediately or within hours of an antigen's appearance in the body. Adaptive immunity refers to antigen-specific immune response. The antigen first must be processed and recognized, and then the adaptive immune system creates an army of immune cells specifically designed to attack that antigen. For the adaptive immune system, specificity and sensitivity are provided by a large repertoire of antigen T-cell receptors (TCRs) constructed in their extracellular domain to recognize antigenic peptide fragments restricted and presented by histocompatibility complex molecules, and coupled through intracellular domains to signal transduction modules that serve to transmit environmental cues inside the cell.

Inflammation is triggered when innate immune cells detect infection or tissue injury. Pattern recognition receptors (PRRs) respond to pathogen-associated molecular patterns (PAMPs) or host-derived damage-associated molecular patterns (DAMPs) by triggering activation of NF-κB, AP1, CREB, c/EBP, and IRF transcription factors. Induction of genes encoding enzymes, chemokines, cytokines, adhesion molecules, and regulators of the extracellular matrix promotes the recruitment and activation of leukocytes. Besides resolving infection and injury, chronic inflammation is a risk factor for cancer.

Immunity has a major impact on inflammatory diseases and cancer, and biologics targeting immune cells and their factors. Immunosuppressant drugs suppress, or reduce, the strength of the body’s immune system, and have been used in the treatment of organ transplantation or autoimmunine diseases. Immunomodulator drugs have contributed to the significant improvement against cancer and other related diseases.

References:
[1] Sakaguchi S, et al. Immunol Cell Biol. 2012 Mar;90(3):277-87. doi: 10.1038/icb.2012.4.
[2] Newton K, et al. Cold Spring Harb Perspect Biol. 2012 Mar; 4(3): a006049.
[3] Bartneck M. Macromol Biosci. 2017 Apr 6. doi: 10.1002/mabi.201700021.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
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Apoptosis >
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Autophagy >
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Membrane Transporter/Ion Channel >
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Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
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Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
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Vitamin D Related >
VD/VDR
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N-ACETYLNEURAMIN-LACTOSE

6'-Sialyllactose is a sialylated human milk oligosaccharide that can promote the proliferation of bifidobacteria and shaping the gut microbiota. 6'-Sialyllactose also inhibits toll-like receptor 4 signaling and protects against the development of necrotizing enterocolitis[1][2].

  • CAS Number: 35890-39-2
  • MF: C23H39NO19
  • MW: 633.55
  • Catalog: Toll-like Receptor (TLR)
  • Density: 1.72 g/cm3
  • Boiling Point: 1134.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 640.1ºC

-Trimethoxyflavone

6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction[1].

  • CAS Number: 720675-74-1
  • MF: C18H16O5
  • MW: 312.317
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 495.2±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 220.3±28.8 °C

STING agonist-25

STING agonist-25 (CF505) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains[1].

  • CAS Number: 2408723-10-2
  • MF: C36H41N13O6
  • MW: 751.79
  • Catalog: STING
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Manelimab

Manelimab is a monoclonal antibody that inhibits programmed death-ligand 1 (PD-L1)[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ODN TTAGGG

ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'[1][2].

  • CAS Number: 1801724-76-4
  • MF:
  • MW:
  • Catalog: Toll-like Receptor (TLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FICZ

FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.

  • CAS Number: 172922-91-7
  • MF: C19H12N2O
  • MW: 284.31
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 463.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 191.1±34.1 °C

StemRegenin 1 (SR1)

StemRegenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.

  • CAS Number: 1227633-49-9
  • MF: C24H23N5OS
  • MW: 429.537
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 622.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 330.5±34.3 °C

CXCR4 probe 1

CXCR4 probe 1 (compound 5) is a potent and specific CXCR4-targeted PET tracer with an IC50 value of 6.9 nM against CXCR4-specific antagonist peptide, TN14003. CXCR4 probe 1 has potential to be used as CXCR4-specific imaging probe to diagnose and monitor the prognosis of inflammatory diseases, CXCR4-positive tumors, and metastatic cancers[1].

  • CAS Number: 2077985-50-1
  • MF: C24H3018FN5O4S
  • MW: 502.59
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SB 265610

SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively[1][2].

  • CAS Number: 211096-49-0
  • MF: C14H9BrN6O
  • MW: 357.16500
  • Catalog: CXCR
  • Density: 1.779 g/cm3
  • Boiling Point: 527ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 272.5ºC

Avizakimab

Avizakimab (BOS161721) is a humanized IgG1 monoclonal antibody that targets interleukin-21[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

trans-Isoferulic acid-d3

trans-Isoferulic acid-d3 is the deuterium labeled trans-Isoferulic acid[1]. trans-Isoferulic acid (trans-3-Hydroxy-4-methoxycinnamic acid) is an aromatic acid isolated from the roots of Clematis florida var. plena. trans-Isoferulic acid exhibits anti-inflammatory activity[2].trans-isoferulic acid suppresses NO and PGE2 production through the induction of Nrf2-dependent heme oxygenase-1 (HO-1)[3].

  • CAS Number: 1028203-97-5
  • MF: C10H7D3O4
  • MW: 197.20200
  • Catalog: Prostaglandin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Plerixafor 8HCl (AMD3100 8HCl)

Plerixafor octahydrochloride is a selective CXCR4 antagonist with an IC50 of 44 nM.

  • CAS Number: 155148-31-5
  • MF: C28H62Cl8N8
  • MW: 830.500
  • Catalog: CXCR
  • Density: 0.962g/cm3
  • Boiling Point: 657.5ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 361.8ºC

Mirikizumab

Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody targets the p19 subunit of interleukin 23. Mirikizumab can be used for the research of ulcerative colitis[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Licofelone

Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor for the treatment of osteoarthritis. Licofelone (ML-3000) exerts anti-inflammatory and anti-proliferative effects. Licofelone (ML-3000) induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[1][2].

  • CAS Number: 156897-06-2
  • MF: C23H22ClNO2
  • MW: 379.879
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 539.7±50.0 °C at 760 mmHg
  • Melting Point: 162-163ºC
  • Flash Point: 280.2±30.1 °C

7-Ethoxyresorufin

7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate for and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].

  • CAS Number: 5725-91-7
  • MF: C14H11NO3
  • MW: 241.242
  • Catalog: NO Synthase
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 389.3±42.0 °C at 760 mmHg
  • Melting Point: 223-225ºC(lit.)
  • Flash Point: 185.9±22.3 °C

Kansuinine B

Kansuinine B inhibits IL-6-induced Stat3 activation. Kansuinine B possesses anti-viral activity and could be used in the study for COVID-19[1][2][3].

  • CAS Number: 57685-46-8
  • MF: C38H42O14
  • MW: 722.73200
  • Catalog: SARS-CoV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TLR7/8 agonist 1 dihydrochloride

TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.

  • CAS Number: 1620278-72-9
  • MF: C22H27Cl2N5
  • MW: 432.39
  • Catalog: Toll-like Receptor (TLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Quetmolimab

Quetmolimab is a humanized anti-CX3CL1 monoclonal antibody. However, CX3CL1 is a chemokine with a modulating effect on chemotaxis and adhesion[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

STING agonist-11

STING agonist-11 (Compound 92) is a potent small molecule cyclic urea activator of STING with EC50 of 18 nM. Activation of STING is a highly promising approach in immunotherapy[1].

  • CAS Number: 2259308-68-2
  • MF: C25H20ClF4N3O2
  • MW: 505.89
  • Catalog: STING
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ac-Tyr-Val-Ala-Asp-aldehyde (pseudo acid)

Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO can suppress the production of mature IL-lβ[1].

  • CAS Number: 143313-51-3
  • MF: C23H32N4O8
  • MW: 492.522
  • Catalog: Interleukin Related
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 937.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 520.9±34.3 °C

Elubrixin

Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation[1][2][3].

  • CAS Number: 688763-64-6
  • MF: C17H17Cl2FN4O4S
  • MW: 463.31100
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IAXO-102

IAXO-102 is a TLR4 antagonist, inhibits MAPK and p65 NF-kB phosphorylation involved in down regulation of the expression of TLR4 and TLR4 dependent proinflammatory protein. IAXO-102 prevents experimental abdominal aortic aneurysm development[1].

  • CAS Number: 1115270-63-7
  • MF: C35H71NO5
  • MW: 585.94
  • Catalog: Toll-like Receptor (TLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Vobarilizumab

Vobarilizumab (ALX-0061) is an anti-IL-6R monoclonal antibody (mAb) (Kd: 0.19 pM). Vobarilizumab consists of an anti-IL-6R domain and an anti-human serum albumin domain. Vobarilizumab can be used in the research of inflammatory autoimmune diseases, such as rheumatoid arthritis[1][2][3].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-5

PROTAC IRAK4 degrader-5 is a PROTAC-based IRAK4 degrader extracted from patent US20190192668A1, compound I-171[1].

  • CAS Number: 2360530-61-4
  • MF: C41H40F3N11O9
  • MW: 887.82
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pacmilimab

Pacmilimab (CX-072) is a potent PD-L1 inhibitor. Pacmilimab shows antitumor activity[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

C5aR-IN-2

C5aR-IN-2 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-2 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 49)[1].

  • CAS Number: 2761048-06-8
  • MF: C36H40FN5O2
  • MW: 593.73
  • Catalog: Complement System
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Irdabisant

Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment[1][2].

  • CAS Number: 1005402-19-6
  • MF: C18H23N3O2
  • MW: 313.394
  • Catalog: Histamine Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lusutrombopag

Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.

  • CAS Number: 1110766-97-6
  • MF: C29H32Cl2N2O5S
  • MW: 591.546
  • Catalog: Thrombopoietin Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IL-17A modulator-1

IL-17A modulator-1 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 9. IL-17A modulator-1 inhibits the biological action of IL-17A with a pIC50 of 8.2. IL-17A modulator-1 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders[1].

  • CAS Number: 2748749-29-1
  • MF: C33H31N5O4
  • MW: 561.63
  • Catalog: Interleukin Related
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TLR4-IN-C34-C2-COOH

TLR4-IN-C34-C2-COO is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis[1].

  • CAS Number: 1159408-54-4
  • MF: C19H29NO11
  • MW: 447.43
  • Catalog: Toll-like Receptor (TLR)
  • Density: 1.29±0.1 g/cm3(Predicted)
  • Boiling Point: 634.1±55.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: 337.3±31.5 °C