A-943931 HCL | CAS# 1227675-50-4 (HCl) | Potent and selective H4 antagonist

A-943931 HCL
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 581019

CAS#: 1227675-50-4 (HCL)

Description: A-943931 is a potent and selective histamine H4 receptor antagonist in functional assays across species (FLIPR Ca (2+) flux, K b < 5.7 nM), has high (>190x) selectivity for H 4, and combines good PK in rats and mice (t 1/2 of 2.6 and 1.6 h, oral bioavailability of 37% and 90%) with anti-inflammatory activity (ED 50 = 37 micromol/kg, mouse) and efficacy in pain models (thermal hyperalgesia, ED 50 = 72 micromol/kg, rat). Blocks inflammation in a peritonitis mouse model and displays efficacy in inflammatory pain and neuropathic pain models. Shows anti-inflammatory and analgesic effects in vivo. Orally active.

Chemical Structure

A-943931 HCL

CAS# 1227675-50-4 (HCL)

Instruction

Theoretical Analysis

MedKoo Cat#: 581019
Name: A-943931 HCL
CAS#: 1227675-50-4 (HCL)
Chemical Formula: C17H23Cl2N5
Exact Mass: 295.18
Molecular Weight: 368.310
Elemental Analysis: C, 55.44; H, 6.29; Cl, 19.25; N, 19.02

Price and Availability

Size	Price	Availability
10mg	USD 380	2 Weeks
50mg	USD 1160	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 1227675-50-4 (HCL); 1227675-50-4

Synonym: A-943931 Dihydrochloride; A-943931 HCL; A 943931 HCI; A-943931(HCL); A-943931-HCI; A-943931Dihydrochloride; A 943931 Dihydrochloride; A-943931-Dihydrochloride, A943931Dihydrochloride.

IUPAC/Chemical Name: (R)-4-(3-aminopyrrolidin-1-yl)-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-amine dihydrochloride

InChi Key: ISYUFRNZHUOGLA-CURYUGHLSA-N

InChi Code: InChI=1S/C17H21N5.2ClH/c18-12-8-9-22(10-12)16-14-7-3-5-11-4-1-2-6-13(11)15(14)20-17(19)21-16;;/h1-2,4,6,12H,3,5,7-10,18H2,(H2,19,20,21);2*1H/t12-;;/m1../s1

SMILES Code: NC1=NC(N2C[C@H](N)CC2)=C(CCCC3=CC=CC=C34)C4=N1.[H]Cl.[H]Cl

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

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 368.31 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:
In vitro protocol:
In vivo protocol:

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1: Cowart MD, Altenbach RJ, Liu H, Hsieh GC, Drizin I, Milicic I, Miller TR,
Witte DG, Wishart N, Fix-Stenzel SR, McPherson MJ, Adair RM, Wetter JM,
Bettencourt BM, Marsh KC, Sullivan JP, Honore P, Esbenshade TA, Brioni JD.
Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class
of histamine H4 receptor antagonists with improved druglikeness and in vivo
efficacy in pain and inflammation models. J Med Chem. 2008 Oct 23;51(20):6547-57.
doi: 10.1021/jm800670r. Epub 2008 Sep 26. PubMed PMID: 18817367.

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A-943931 HCL featured