BMS-933043

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MedKoo CAT#: 530504

CAS#: 1221973-93-8

Description: 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

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BMS-933043
CAS# 1221973-93-8
Instruction

Theoretical Analysis

MedKoo Cat#: 530504
Name: BMS-933043
CAS#: 1221973-93-8
Chemical Formula: C16H19N7O
Exact Mass: 325.17
Molecular Weight: 325.376
Elemental Analysis: C, 59.06; H, 5.89; N, 30.13; O, 4.92

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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:

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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