2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. BMS-986121

BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs.

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BMS-986121 Chemical Structure

BMS-986121 Chemical Structure

CAS No. : 313671-26-0

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Customer Review

Based on 1 publication(s) in Google Scholar

BMS-986121 Related Antibodies

Top Publications Citing Use of Products

View All Opioid Receptor Isoform Specific Products:

View All Isoforms
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs[1][2][3].

IC50 & Target

μ Opioid Receptor/MOR

 

In Vitro

BMS-986121 (1 μM~1 mM) significantly augments the β-arrestin–recruitment response produced by a low concentration of endomorphin-I (PAM-detection mode). BMS-986121 significantly increases the inhibition of forskolin-stimulated adenylyl cyclase activity produced by a ∼EC10 (30 pM) concentration of endomorphin-I in CHOμ cells. BMS-986121 (100 μM) produces leftward shifts in the potency of endomorphin-I (fourfold) and leu-enkephalin (sixfold), in inhibition of forskolin-stimulated cAMP-accumulation assays in CHO-μ cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-986121 Related Antibodies
Molecular Weight

366.22

Formula

C15H9Cl2N3O2S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=[N+](C1=CC=C(C2=CSC(NC3=C(Cl)C=CC=C3Cl)=N2)C=C1)[O-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (273.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7306 mL 13.6530 mL 27.3060 mL
5 mM 0.5461 mL 2.7306 mL 5.4612 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7306 mL 13.6530 mL 27.3060 mL 68.2650 mL
5 mM 0.5461 mL 2.7306 mL 5.4612 mL 13.6530 mL
10 mM 0.2731 mL 1.3653 mL 2.7306 mL 6.8265 mL
15 mM 0.1820 mL 0.9102 mL 1.8204 mL 4.5510 mL
20 mM 0.1365 mL 0.6826 mL 1.3653 mL 3.4132 mL
25 mM 0.1092 mL 0.5461 mL 1.0922 mL 2.7306 mL
30 mM 0.0910 mL 0.4551 mL 0.9102 mL 2.2755 mL
40 mM 0.0683 mL 0.3413 mL 0.6826 mL 1.7066 mL
50 mM 0.0546 mL 0.2731 mL 0.5461 mL 1.3653 mL
60 mM 0.0455 mL 0.2275 mL 0.4551 mL 1.1377 mL
80 mM 0.0341 mL 0.1707 mL 0.3413 mL 0.8533 mL
100 mM 0.0273 mL 0.1365 mL 0.2731 mL 0.6826 mL
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BMS-986121 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-986121313671-26-0BMS986121BMS 986121Opioid ReceptorpositiveallostericchemicalscaffoldchemotypePAMsInhibitorinhibitorinhibit

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