WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H526679
CAS#: 199864-87-4 (free base)
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).
Hodoodo Cat#: H526679
Name: RS-127445
CAS#: 199864-87-4 (free base)
Chemical Formula: C17H16FN3
Exact Mass: 281.13
Molecular Weight: 281.334
Elemental Analysis: C, 72.58; H, 5.73; F, 6.75; N, 14.94
Related CAS #: 199864-86-3 (HCl) 199864-87-4 (free base) 199864-88-5 (maleate)
Synonym: RS-127445; RS 127445; RS127445; MT-500; MT 500; MT500.
IUPAC/Chemical Name: 2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine
InChi Key: ZZZQXCUPAJFVBN-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: CC(C1=CC(C2=C3C=CC=CC3=C(F)C=C2)=NC(N)=N1)C
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
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The following data is based on the product molecular weight 281.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
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1. Bassil AK, Taylor CM, Bolton VJ, Gray KM, Brown JD, Cutler L, Summerfield SG, Bruton G, Winchester WJ, Lee K, Sanger GJ. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. Br J Pharmacol. 2009 Sep;158(1):252-8. doi: 10.1111/j.1476-5381.2009.00155.x. Epub 2009 Apr 9. PMID: 19371340; PMCID: PMC2795249.
2: Bonhaus DW, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, Chang LK, Pulido-Rios T, Webber A, Leung E, Eglen RM, Martin GR. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127(5):1075-82. PubMed PMID: 10455251; PubMed Central PMCID: PMC1566110.
