pTH (39-84) (human) is a parathyroid hormone (PTH) C-terminal fragment. pTH (39-84) (human) stimulates osteoclast formation[1].
Suvratoxumab (MEDI4893) is a long-acting, high-affinity humanized anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394)[1][2][3].
DPP1-IN-1 hydrate is a DPP1 inhibitor (IC50: 1.6 nM). DPP1-IN-1 hydrate has good bioavailability and pharmacokinetic characteristics, and can be used for research of inflammatory disease[1].
7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro[1].
Phenylbutazone is used as a non-steroidal anti-inflammatory agent for the treatment of chronic pain, including the symptoms of arthritis.Target: OthersPhenylbutazone was originally made available for use in humans for the treatment of rheumatoid arthritis and gout in 1949. However, when combined with paracetamol and many other household painkillers even in the smallest doses can cause irreversible liver degradation proving fatal in many cases. It is no longer approved, and therefore not marketed, for any human use in the United States. In the UK it is used to treat ankylosing spondylitis, but only when other therapies are unsuitable.Phenylbutazone may be administered orally (via paste, powder or feed-in) or intravenously. It should not be given intramuscularly or injected in any place other than a vein, as it can cause tissue damage. Tissue damage and edema may also occur if the drug is injected repetitively into the same vein. Phenylbutazone should be administered only under the advice of a veterinarian.
4α-Phorbol 12,13-didecanoate (4αPDD) is a TRPV4 agonist with antidipsogenic effects. 4α-Phorbol 12,13-didecanoate promotes Ca2+ influx[1].
NLRP3 modulators 1 is the potent modulator of NLRP3. NLRP3 modulators 1 agonizes or partially agonizes NLRP3 that are useful for researching a condition, disease or disorder in which a decrease in LRP3 activity contributes to the pathology (extracted from patent WO2017184746A1, compound 107)[1].
Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria. Target: Histamine H1 ReceptorBilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors [1]. Bilastine distribution has an apparent volume of distribution of 1.29 L/kg, and has an elimination half-life of 14.5 h and plasma protein binding of 84-90% [2].
KC01 is a potent and selective inhibitor of ABHD16A with IC50 of 90 nM for hABHD16A, 520 nM for mABHD16A; shows significant reductions in all detected cellular lyso-PSs, no activity in other lipids, including PSs, PCs, PEs, lyso-PCs, lyso-PEs, or monoacylglycerols (MAGs); decreases both lyso-PSs and lipopolysaccharide-induced cytokine production in mouse macrophages.
Cauloside C is a triterpene glycoside isolated from Caulophyllum robustum Max. Cauloside C exerts anti-inflammatory effects through the inhibition of expression of iNOS and proinflammatory cytokines[1].
Echinocystic acid a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties. In vitro: Echinocystic acid (EA) inhibit the formation of osteoclast. EA inhibit RANKL-induced NF-κB activation and ERK phosphorylation in BMMs. [1] EA inhibit IL-1β-induced inflammation in chondrocytes. [2]In vivo: Echinocystic acid reduces reserpine-induced pain/depression dyad in mice. [3]
Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal is a glucocorticoid receptor agonist. Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used in anti-CD40 antibody drug conjugate (ADC). Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used for the research of inflammation and immune regulation[1].
PPM-18 (NSC 73233), a potent anti-inflammatory agent, inhibits nitric oxide synthase expression. PPM-18 is a potent inhibitor of iNOS expression by blocking the binding of NF-κB to promoter[1]. PPM-18, an analog of Vitamin K, induces autophagy and apoptosis in bladder cancer cells through ROS and AMPK signaling pathways[2].
Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis[1][2][3].
HP210 is a selective glucocorticoid receptor modulator (SGRM). HP210 can inhibit the mRNA expression of IL-1β and IL-6. HP210 has the potential to study inflammation-related diseases[1].
Rimexolone (Org 6216) is a glucocorticoid steroid with anti-inflammatory activity. Rimexolone can be used as a 1% ophthalmic suspension for the management of ocular inflammation[1][2].
MrgprX2 antagonist-4 is an MrgprX2 antagonist extracted from patent US20210128561A1, compound B-51 E117. MrgprX2 antagonist-4 can be used for the research of inflammatory disorders of the skin[1].
Sciadopitysin is a type of biflavonoids in leaves from ginkgo biloba[1]. Sciadopitysi inhibits RANKL-induced osteoclastogenesis and bone loss by inhibiting NF-κB activation and reducing the expression of c-Fos and NFATc1[2].
GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.
Autotaxin-IN-4 (compound 51), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-4 has the potential to treat idiopathic pulmonary fibrosis[1].
HJM-561 is a potent, selective, orally bioavailable EGFR PROTAC. HJM-561 overcomes osimertinib (HY-15772)-resistant EGFR triple mutations and has anti-tumor activity[1].
Cletoquine oxalate (Desethylhydroxychloroquine oxalate) is a major active metabolite of Hydroxychloroquine. Cletoquine oxalate is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine oxalate is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine oxalate has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
CZL55 is a caspase-1 inhibitor with an IC50 value of 24 nM. CZL55 can be used for the research of febrile seizures (FS)[1].
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research[1][2][3][4].
Cimifugin is a major components of Yu-ping-feng-san, a Chinese medical formula that is used clinically for allergic diseases and characterized by reducing allergy relapse.
EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research[1].
Alphitolic acid (Aophitolic acid) is an anti-inflammatory triterpene could found in quercus aliena. Alphitolic acid blocks Akt–NF-κB signaling to induce apoptosis. Alphitolic acid induces autophagy. Alphitolic acid has anti-inflammatory activity and down-regulates the NO and TNF-α production. Alphitolic acid can be used for cancer and inflammation research[1][2][3].
Glucosamine-15N hydrochloride is the 15N labeled Glucosamine hydrochloride. Glucosamine hydrochloride (D-Glucosamine hydrochloride) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a
Praeroside IV can be isolated from the roots of Angelica furcijuga. Praeroside IV can be used for research of D-GalN/LPS-induced liver injury[1].
Aureobasidin A (Basifungin), a cyclic depsipetide, is an antifungal antibiotic. Aureobasidin A (Basifungin) A is an inhibitor of the inositolphosphorylceramide synthase AUR1[1][2].