BMS-986163

Alias: Prodrug of BMS-986169; BMS-986163; BMS 986163; BMS986163.
Cat No.:V3464 Purity: ≥98%
BMS-986163, a novel water-soluble phosphate prodrug ofBMS-986169designed for IV administration, is a negative allosteric modulator ofGluN2B which is aN-methyl-d-aspartate receptor subtype.
BMS-986163 Chemical Structure CAS No.: 1801151-09-6
Product category: Others 8
This product is for research use only, not for human use. We do not sell to patients.
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10mg
25mg
50mg
100mg
250mg

Other Forms of BMS-986163:

  • BMS-986169
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

BMS-986163, a novel water-soluble phosphate prodrug of BMS-986169 designed for IV administration, is a negative allosteric modulator of GluN2B which is a N-methyl-d-aspartate receptor subtype. The prodrug BMS-986163 can be rapidly convertd to its active form BMS-986169 which has Ki of 4 nM and IC50 of 24 nM. BMS-986163 has potential to be used in major depressive disorder. BMS-986169 exhibited high binding affinity for the GluN2B allosteric site (Ki = 4.0 nM) and selective inhibition of GluN2B receptor function (IC50 = 24 nM) in cells. The conversion of prodrug BMS-986163 to parent BMS-986169 was rapid in vitro and in vivo across preclinical species. The prodrug BMS-986163 has demonstrated an acceptable safety and toxicology profile and was selected as a preclinical candidate for further evaluation in major depressive disorder.

Biological Activity I Assay Protocols (From Reference)
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H28FN2O5P
Molecular Weight
462.45099067688
CAS #
1801151-09-6
SMILES
O=C1N(CC2=CC=C(C)C=C2)CC[C@H]1N3C[C@@H](F)[C@H](C4=CC=C(OP(O)(O)=O)C=C4)CC3
InChi Key
ZPUVTBAQHJFPHE-BHDDXSALSA-N
InChi Code
InChI=1S/C23H28FN2O5P/c1-16-2-4-17(5-3-16)14-26-13-11-22(23(26)27)25-12-10-20(21(24)15-25)18-6-8-19(9-7-18)31-32(28,29)30/h2-9,20-22H,10-15H2,1H3,(H2,28,29,30)/t20-,21+,22+/m0/s1
Chemical Name
4-((3S,4S)-3-fluoro-1-((R)-1-(4-methylbenzyl)-2-oxopyrrolidin-3-yl)piperidin-4-yl)phenyl dihydrogen phosphate
Synonyms
Prodrug of BMS-986169; BMS-986163; BMS 986163; BMS986163.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1624 mL 10.8120 mL 21.6240 mL
5 mM 0.4325 mL 2.1624 mL 4.3248 mL
10 mM 0.2162 mL 1.0812 mL 2.1624 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
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