| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Purity: ≥98%
| ln Vitro |
BMS-986122 promotes the recruitment of β-arrestin in U2OS-OPRM1 human osteosarcoma cells that express u-opioid receptors in response to endorphin 1 (EC50=3 μM). BMS-986122 upregulates the suppression of forskolin-stimulated adenylyl cyclase activity in CHO cells that express human recombinant u-opioid linkers, which is activated by endorphin 1 (EC50=8.9 μM). In mouse meninges, BMS-986122 increases DAMGO-mediated binding of [35S]GTPγS and, to some extent, seems to be a positive affinity modulator of DAMGO binding via u-opioid uptake [1]. In CHO cells expressing human u-opioid receptors, BMS-986122 enhances the ability of the endogenous opioid methionine-enkephalin (Met-Enk) to stimulate G protein activity, while it is inactive on its own and less effective than β-arrestin Enhanced G-protein activation recruitment. BMS-986122 amplifies Met-Enk's ability to suppress GABA release in the periaqueductal gray matter, a critical area for anti-injury effects [2]. BMS-986122 possesses the similarly related δ-OR and is selective for μ-OR. A quiet allosteric modulator of δ-OR and κ-OR is BMS-986122 [3].
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| References |
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| Molecular Formula |
C16H15BRCLNO3S2
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|---|---|
| Molecular Weight |
448.782200098038
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| Exact Mass |
446.936
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| CAS # |
313669-88-4
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| PubChem CID |
4644453
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
567.2±60.0 °C at 760 mmHg
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| Flash Point |
296.8±32.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.648
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| LogP |
5.14
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
522
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1CCN(S(C2=CC=C(Cl)C=C2)(=O)=O)C1C1=CC=C(OC)C(Br)=C1
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| InChi Key |
PNGJPVDGZNPZHY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15BrClNO3S2/c1-22-15-7-2-11(10-14(15)17)16-19(8-9-23-16)24(20,21)13-5-3-12(18)4-6-13/h2-7,10,16H,8-9H2,1H3
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| Chemical Name |
2-(3-bromo-4-methoxyphenyl)-3-(4-chlorophenyl)sulfonyl-1,3-thiazolidine
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| Synonyms |
BMS-986122 BMS 986122 BMS986122.
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~222.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.57 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2283 mL | 11.1413 mL | 22.2826 mL | |
| 5 mM | 0.4457 mL | 2.2283 mL | 4.4565 mL | |
| 10 mM | 0.2228 mL | 1.1141 mL | 2.2283 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.
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.
(2) Be sure to add the solvent(s) in order.
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