MedKoo Cat#: 530504 | Name: BMS-933043

Description:

WARNING: This product is for research use only, not for human or veterinary use.

BMS-933043 is a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia. BMS-933043 showed potent binding affinity to native rat (Ki = 3.3 nM) and recombinant human alpha7 nicotinic acetylcholine receptors (Ki = 8.1 nM) and agonist activity in a calcium fluorescence assay (EC50 = 23.4 nM) and whole cell voltage clamp electrophysiology (EC50 = 0.14 micromolar (rat) and 0.29 micromolar (human)). BMS-933043 showed no agonist or antagonist activity at other nicotinic acetylcholine receptor subtypes and was at least 300 fold weaker at binding to and antagonizing human 5-HT3A receptors (Ki = 2,451 nM; IC50 = 8,066 nM).

Chemical Structure

BMS-933043
CAS#1221973-93-8

Theoretical Analysis

MedKoo Cat#: 530504

Name: BMS-933043

CAS#: 1221973-93-8

Chemical Formula: C16H19N7O

Exact Mass: 325.1651

Molecular Weight: 325.38

Elemental Analysis: C, 59.06; H, 5.89; N, 30.13; O, 4.92

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
BMS-933043; BMS 933043; BMS933043.
IUPAC/Chemical Name
(2R)-N-(6-(1H-imidazol-1-yl)-4-pyrimidinyl)-4'H-spiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxazol]-2'-amine
InChi Key
RLXBHTUZCPORKT-INIZCTEOSA-N
InChi Code
InChI=1S/C16H19N7O/c1-4-22-5-2-12(1)16(9-22)8-18-15(24-16)21-13-7-14(20-10-19-13)23-6-3-17-11-23/h3,6-7,10-12H,1-2,4-5,8-9H2,(H,18,19,20,21)/t16-/m0/s1
SMILES Code
C1(CC2)[C@@]3(OC(NC4=NC=NC(N5C=CN=C5)=C4)=NC3)CN2CC1
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

Preparing Stock Solutions

The following data is based on the product molecular weight 325.38 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.

Recalculate based on batch purity %
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
1: Bristow LJ, Easton AE, Li YW, Sivarao DV, Lidge R, Jones KM, Post-Munson D, Daly C, Lodge NJ, Gallagher L, Molski T, Pieschl R, Chen P, Hendricson A, Westphal R, Cook J, Iwuagwu C, Morgan D, Benitex Y, King D, Macor JE, Zaczek R, Olson R. The Novel, Nicotinic Alpha7 Receptor Partial Agonist, BMS-933043, Improves Cognition and Sensory Processing in Preclinical Models of Schizophrenia. PLoS One. 2016 Jul 28;11(7):e0159996. doi: 10.1371/journal.pone.0159996. PubMed PMID: 27467081; PubMed Central PMCID: PMC4965148. 2. BMS-933043, a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia Dalton KingChristiana IwuagwuJim CookIvar M. McDonaldRobert MateF. Christopher ZusiMatthew D. HillHaiquan FangRulin ZhaoBei WangAmy E. EastonRegina MillerDebra Post-MunsonRonald J. KnoxLizbeth GallagherRyan WestphalThaddeus MolskiJingsong FanWendy ClarkeYulia BenitexKimberley A. LentzRex DentonDaniel MorganRobert ZaczekNicholas J. LodgeLinda J. BristowJohn E. MacorRichard E. Olson Publication Date (Web): February 8, 2017 (Letter) DOI: 10.1021/acsmedchemlett.7b00032