G Protein Coupled Receptors (GPCRs) perceive many extracellular signals and transduce them to heterotrimeric G proteins, which further transduce these signals intracellular to appropriate downstream effectors and thereby play an important role in various signaling pathways. G proteins are specialized proteins with the ability to bind the nucleotides guanosine triphosphate (GTP) and guanosine diphosphate (GDP). In unstimulated cells, the state of G alpha is defined by its interaction with GDP, G beta-gamma, and a GPCR. Upon receptor stimulation by a ligand, G alpha dissociates from the receptor and G beta-gamma, and GTP is exchanged for the bound GDP, which leads to G alpha activation. G alpha then goes on to activate other molecules in the cell. These effects include activating the MAPK and PI3K pathways, as well as inhibition of the Na+/H+ exchanger in the plasma membrane, and the lowering of intracellular Ca2+ levels.

Most human GPCRs can be grouped into five main families named; Glutamate, Rhodopsin, Adhesion, Frizzled/Taste2, and Secretin, forming the GRAFS classification system.

A series of studies showed that aberrant GPCR Signaling including those for GPCR-PCa, PSGR2, CaSR, GPR30, and GPR39 are associated with tumorigenesis or metastasis, thus interfering with these receptors and their downstream targets might provide an opportunity for the development of new strategies for cancer diagnosis, prevention and treatment. At present, modulators of GPCRs form a key area for the pharmaceutical industry, representing approximately 27% of all FDA-approved drugs.

References:
[1] Moreira IS. Biochim Biophys Acta. 2014 Jan;1840(1):16-33.
[2] Tuteja N. Plant Signal Behav. 2009 Oct;4(10):942-7.
[3] Williams C, et al. Methods Mol Biol. 2009;552:39-50.
[4] Schiöth HB, et al. Gen Comp Endocrinol. 2005 May 15;142(1-2):94-101.
[5] Wu J, et al. Cancer Genomics Proteomics. 2012 Jan;9(1):37-50.


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C-Type Natriuretic Peptide (1-53) (human) acetate salt

C-Type Natriuretic Peptide (1-53), human is the 1-53 fragment of C-Type Natriuretic Peptide. C-Type Natriuretic Peptide is natriuretic peptide family peptide that is involved in the maintenance of electrolyte-fluid balance and vascular tone[1].

  • CAS Number: 141294-77-1
  • MF:
  • MW:
  • Catalog: Angiotensin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NTNCB hydrochloride

NTNCB (Compound 11) hydrochloride is a potent and selective neuropeptide Y Y5 (NPY Y5) receptor antagonist with a Ki of 8 nM against human Y5[1].

  • CAS Number: 191931-56-3
  • MF: C25H34ClN3O4S
  • MW: 508.073
  • Catalog: Neuropeptide Y Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Galnon

Galnon is a selective and non-peptide agonist of galanin GAL1 and GAL2 receptor, with Kis of 11.7 and 34.1 μM respectively. Galnon exhibits anticonvulsant and anxiolytic effects[1][2].

  • CAS Number: 475115-35-6
  • MF: C40H46N4O6
  • MW: 678.82
  • Catalog: Neuropeptide Y Receptor
  • Density: 1.242g/cm3
  • Boiling Point: 937.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 520.8ºC

FP0429

FP0429 is a full mGlu4 agonist and partial mGlu8 agonist with EC50 values of 48.3 μM and 56.2 μM, respectively[1].

  • CAS Number: 870860-41-6
  • MF: C10H12N2O7
  • MW: 272.21
  • Catalog: mGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TCB-2

TCB2 is an agonist of serotonin 5-HT2A receptor.

  • CAS Number: 912342-28-0
  • MF: C11H15Br2NO2
  • MW: 353.05000
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dihydro Ergotamine Mesylate

Dihydroergotamine mesylate is an ergot alkaloid used to treat migraines.Target: 5-HT ReceptorsDihydroergotamine is not as effective as sumatriptan or phenothiazines as a single agent for treatment of acute migraine headache; however, when administered with an antiemetic, dihydroergotamine appears to be as effective as opiates, ketorolac, or valproate. Given its nonnarcotic properties, parenteral dihydroergotamine combined with an antiemetic should be considered as effective initial therapy in clinical practice [1]. The introduction of the intranasal formulation of DHE provides both pharmacologic and patient-convenience advantages for use in migraine therapy [2, 3].

  • CAS Number: 6190-39-2
  • MF: C34H41N5O8S
  • MW: 679.783
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: 1001.8ºC at 760 mmHg
  • Melting Point: 232°C
  • Flash Point: 559.7ºC

Vasopressin V2 receptor antagonist 1

Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM. Vasopressin V2 receptor antagonist 1 can be used for autosomal dominant polycystic kidney disease (ADPKD) research[1].

  • CAS Number: 2648650-50-2
  • MF: C33H37ClN4O4
  • MW: 589.12
  • Catalog: Vasopressin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(3β,7α)-Cholest-5-ene-3,7,25-triol

7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells[1][2].

  • CAS Number: 64907-22-8
  • MF: C27H46O3
  • MW: 418.652
  • Catalog: EBI2/GPR183
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 548.5±35.0 °C at 760 mmHg
  • Melting Point: 235 - 236 °C
  • Flash Point: 230.5±20.5 °C

Exendin Fragment 9-39

Exendin (9-39) is a specific and competitive glucagon-like peptide-1 receptor antagonist.

  • CAS Number: 133514-43-9
  • MF: C149H234N40O47S
  • MW: 3369.757
  • Catalog: Peptides
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Olmesartan impurity

Olmesartan impurity is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist has the potential for high blood pressure study[1][2].

  • CAS Number: 154709-18-9
  • MF: C33H26N4O
  • MW: 494.58600
  • Catalog: Angiotensin Receptor
  • Density: 1.17g/cm3
  • Boiling Point: 724.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 392.1ºC

Trimazosin

Trimazosin is an orally active, quinazoline derivative which is structurally related to prazosin. Trimazosin shows hypotensive effect by selectively block α1-adrenoceptors[1][2].

  • CAS Number: 35795-16-5
  • MF: C20H29N5O6
  • MW: 435.47
  • Catalog: Adrenergic Receptor
  • Density: 1.31g/cm3
  • Boiling Point: 648.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 345.8ºC

LTB4 antagonist 3

LTB4 antagonist 3 (compound 24e) is a leukotriene B4 (LTB4) antagonist with an IC50 value of 477 nM. LTB4 antagonist 3 has anti-inflammatory activity[1].

  • CAS Number: 2929239-87-0
  • MF: C29H27NO6
  • MW: 485.53
  • Catalog: Leukotriene Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-MPMDQ

2-MPMDQ is a potent and selective α1-adrenoceptor (Ki=0.37 nM) antagonist over α2-adrenoceptor (Ki=1740 nM). 2-MPMDQ is potent anti-hypertensive agent and has the potential for hypertension research[1].

  • CAS Number: 149847-77-8
  • MF: C23H27N5O2
  • MW: 405.49
  • Catalog: Adrenergic Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 578.2±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 303.5±32.9 °C

PGN36

PGN36 (Compound 18) is a selective cannabinoid CB2 receptor (CB2R) antagonist with a Ki of 0.09 µM[1].

  • CAS Number: 1564253-75-3
  • MF: C21H23N3O3
  • MW: 365.43
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CP-195543

CP-195543 is a potent, selective and orally active leukotriene B4 (LTB4) receptor antagonist with IC50s of 6.8, 37.0 nM for human neutrophils and murine spleen membranes, respectively. CP-195543 blocks CD11b up-regulation. CP-195543 inhibits LTB4-mediated neutrophil infiltration[1].

  • CAS Number: 204981-48-6
  • MF: C24H19F3O4
  • MW: 428.40000
  • Catalog: Leukotriene Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GLP-1R agonist 3

GLP-1R agonist 3 is a potent agonist of GLP-1R. GLP-1R agonist 3 is a thickened imidazole derivative compound. Glucagon-like peptide-1 (GLP-1) is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 3 has the potential for the research of diabetes (extracted from patent WO2021197464A1, compound 1)[1].

  • CAS Number: 2428640-18-8
  • MF: C31H28FN5O4
  • MW: 553.58
  • Catalog: Glucagon Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Neuropeptide Y(29-64)

Neuropeptide Y(29-64) is a 36 amino acid peptide, a fragment of Neuropeptide Y.

  • CAS Number: 303052-45-1
  • MF: C189H284N54O58S
  • MW: 4272.7
  • Catalog: Peptides
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Elisartan

Elisartan is an orally active non-peptide pro-drug of angiotensin II AT1 receptor antagonist HN-12206, and shows anti-hypertension activities.

  • CAS Number: 149968-26-3
  • MF: C27H29ClN6O5
  • MW: 553.00900
  • Catalog: Angiotensin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Norarecoline Hydrochloride

Guvacoline hydrochloride, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal muscarinic receptors[1][2].

  • CAS Number: 6197-39-3
  • MF: C7H12ClNO2
  • MW: 177.62900
  • Catalog: mAChR
  • Density: N/A
  • Boiling Point: 209.1ºC at 760 mmHg
  • Melting Point: 121-122 ºC
  • Flash Point: 80.2ºC

KRAS G12C inhibitor 38

KRAS G12C inhibitor 38 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 38 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129820A1, compound 171)[1].

  • CAS Number: 2660324-77-4
  • MF: C38H43F3N8O2
  • MW: 700.80
  • Catalog: Ras
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Timiperone

Timiperone has a strong affinity for cerebral dopamine D2 receptor. Timiperone has antipsychotic activity, and inhibits stereotyped behaviour. Timiperone can be used for research of schizophrenia[1][2][3].

  • CAS Number: 57648-21-2
  • MF: C22H24FN3OS
  • MW: 397.50900
  • Catalog: Dopamine Receptor
  • Density: 1.31
  • Boiling Point: 560.8ºC at 760 mmHg
  • Melting Point: 201-203ºC
  • Flash Point: 293ºC

prucalopride

Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.IC50 value: 8.6/8.1 for 5-HT4a/4b(pKi)Target: 5-HT4 receptorPrucalopride is a novel enterokinetic compound and is the first representative of the benzofuran class. Receptor binding data have demonstrated prucalopride's high affinity to both investigated 5-HT(4) receptor isoforms, with mean pK(i) estimates of 8.60 and 8.10 for the human 5-HT(4a) and 5-HT(4b) receptor, respectively. From the 50 other binding assays investigated in this study only the human D(4) receptor (pK(i) 5.63), the mouse 5-HT(3) receptor (pK(i) 5.41) and the human sigma(1) (pK(i) 5.43) have shown measurable affinity, resulting in at least 290-fold selectivity for the 5-HT(4) receptor [1].

  • CAS Number: 179474-81-8
  • MF: C18H26ClN3O3
  • MW: 367.870
  • Catalog: 5-HT Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 481.4±45.0 °C at 760 mmHg
  • Melting Point: 90.7°
  • Flash Point: 244.9±28.7 °C

SCH 54292

SCH54292 is a potent Ras-GEF interaction inhibitor with IC50 of 0.7 μM[1].

  • CAS Number: 188480-51-5
  • MF: C24H28N2O9S
  • MW: 520.552
  • Catalog: Ras
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 810.0±75.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 443.7±37.1 °C

TC-G 1003

sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst2) agonist with a Ki value of 0.025 nM and a cAMP IC50 value of 4.8 nM. sst2 Receptor agonist-1 can inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect[1].

  • CAS Number: 1021912-42-4
  • MF: C26H25ClN2O2
  • MW: 432.94200
  • Catalog: Somatostatin Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ladarixin sodium

A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM; prevents PMN infiltration and tissue damage in several models of IR injury in vivo; abrogates motility and induces apoptosis in cultured cutaneous and uveal melanoma cells and xenografts; also prevents inflammation-mediated damage in MLD-STZ, prevents and reverses diabetes in NOD mice. Diabetes Phase 2 Clinical

  • CAS Number: 865625-56-5
  • MF: C11H11F3NNaO6S2
  • MW: 397.323
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Clonidine

Clonidine is an alpha 2-adrenergic agonist which is used extensively in anesthesia research[1].

  • CAS Number: 4205-90-7
  • MF: C9H9Cl2N3
  • MW: 230.094
  • Catalog: Adrenergic Receptor
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 319.3±52.0 °C at 760 mmHg
  • Melting Point: 141-142℃
  • Flash Point: 146.9±30.7 °C

Neuropeptide Y (1-24) amide (human, rat) trifluoroacetate salt

Neuropeptide Y (1-24) (human) is a neuropeptide with potencies in inhibiting the electricity stimulated twitch response of rat vas deferens. Neuropeptide Y (1-24) (human) stimulates N-methyl-D-aspartate (NMDA)-induced neuronal activation in the rat CA3 region of the dorsal hippocampus in vivo[1][2].

  • CAS Number: 131448-51-6
  • MF: C116H170N30O40S
  • MW: 2656.83000
  • Catalog: Neuropeptide Y Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-Epinephrine-d3

L-Epinephrine-d3 is deuterium labeled L-Epinephrine. L-Epinephrine is a hormone secreted by the medulla of the adrenal glands. L-Epinephrine is an α-adrenergic and β-adrenergic receptor agonist.

  • CAS Number: 1217733-17-9
  • MF: C9H10D3NO3
  • MW: 186.22
  • Catalog: Adrenergic Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KRAS inhibitor-16

KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers[1].

  • CAS Number: 2230873-67-1
  • MF: C20H16Cl2FN3O2S
  • MW: 452.33
  • Catalog: Ras
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KRAS G12C inhibitor 54

KRAS G12C inhibitor 54 (Compound 1) is a KRAS G12C inhibitor[1].

  • CAS Number: 2765580-17-2
  • MF: C36H40F3N7O3S
  • MW: 707.81
  • Catalog: Ras
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A