Product Name :
RS-127445
Description:
RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1, 000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3).
CAS:
199864-87-4
Molecular Weight:
281.33
Formula:
C17H16FN3
Chemical Name:
2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine
Smiles :
CC(C)C1=CC(=NC(N)=N1)C1=CC=C(F)C2=CC=CC=C21
InChiKey:
ZZZQXCUPAJFVBN-UHFFFAOYSA-N
InChi :
InChI=1S/C17H16FN3/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13/h3-10H,1-2H3,(H2,19,20,21)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1, 000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3).|Product information|CAS Number: 199864-87-4|Molecular Weight: 281.33|Formula: C17H16FN3|Synonym:|RS-127445|RS 127445|RS127445|MT-500|MT 500|MT500|Chemical Name: 2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine|Smiles: CC(C)C1=CC(=NC(N)=N1)C1=CC=C(F)C2=CC=CC=C21|InChiKey: ZZZQXCUPAJFVBN-UHFFFAOYSA-N|InChi: InChI=1S/C17H16FN3/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13/h3-10H,1-2H3,(H2,19,20,21)|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO: 56 mg/mL(199.05 mM). Water: Insoluble.|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Anti-Mouse TNF alpha Antibody (TN3-19.12)} site|{Anti-Mouse TNF alpha Antibody (TN3-19.12)} Apoptosis|{Anti-Mouse TNF alpha Antibody (TN3-19.12)} Epigenetics|{Anti-Mouse TNF alpha Antibody (TN3-19.12)} Protocol|{Anti-Mouse TNF alpha Antibody (TN3-19.12)} In Vitro|{Anti-Mouse TNF alpha Antibody (TN3-19.12)} custom synthesis} |Shelf Life: ≥12 months if stored properly.{{Lovastatin} MedChemExpress|{Lovastatin} Ferroptosis|{Lovastatin} Technical Information|{Lovastatin} Description|{Lovastatin} manufacturer|{Lovastatin} Epigenetics} |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:23439434 |Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|RS-127445 is a novel high affinity, selective 5-HT2B receptor antagonist devoid of detectable intrinsic activity. RS-127445 is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor. RS-127445 is thus among the highest affinity, most selective 5- HT2B receptor ligands. RS-127445 potently blocks the 5-HT evoked increase in inositol phosphate formation and blocks the 5-HT evoked increases in intracellular calcium concentrations with a potency 1000 times greater than that of yohimbine.|In Vivo:|RS-127445 is readily absorbed with no obvious dose or route-dependent limitations and rapidly absorbed following both oral and intraperitoneal administration with peak plasma concentrations being achieved within 15 min of dosing. RS-127445 concentration in the plasma are proportional to the administered dose. RS-127445 administrated at dose of 5 mg/kg with approximately 60% of an intraperitoneal dose and 14% of the oral dose is bioavailable. RS-127445 concentration in the plasma is predicted to fully saturate accessible 5-HT2B receptors can be readily achieved and maintained in the rat. RS-127445 administered at 1 to 10 mg/kg with oral significantly inhibits visceral hypersensitivity up to 35 to 74% provoked by restraint stress. Oral RS-127445 produces a significant suppression of TNBS-induced visceral hypersensitivity (15 to 62% inhibition at 3 to 30 mg/ kg), although RS-127445 has no significant effect on the visceral nociceptive threshold of native rats. RS-127445 administrated orally with 1 to 30 mg/kg also dose -dependently reduce the restraint stress-induced defecation in native and TNBS-treated rats. . RS-127445 inhibits colonic motility and defecation.|References:|Bassil AK, et al. Br J Pharmacol, 2009, 158(1), 252-258.Ohashi-Doi K, et al. Neurogastroenterol Motil, 2010, 22(2),e69-e76.Douglas W Bonhaus, et al. Br J Pharmacol, 1999, 127(5), 1075-1082.Products are for research use only. Not for human use.|