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| 25mg |
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Purity: ≥98%
AMG 333 is a novel, potent and highly selective TRPM8 antagonist with an IC50 of 13 nM and 20 nM for hTRPM8 and rTRPM8, respectively. AMG-333can be potentially used for the treatment of migraine. In vitro toxicology profiling showed that AMG-333 was selective over several other TRP channels (IC50 TRPV1, V3, V4 > 20 μM; TRPA1 > 40 μM) and had no hits in off-target-activity panels (CEREP, 144 targets at 10 μM, POC > 45%; Ambit kinase, 100 at 1 μM, POC > 50%). AMG-333 was well-tolerated in 28 day rat and dog preclinical safety studies and advanced to Phase 1 human clinical trials.
| References |
|---|
| Molecular Formula |
C20H12F5N3O4
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|---|---|
| Molecular Weight |
453.319002151489
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| CAS # |
1416799-28-4
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| SMILES |
O=C(O)C1=CN=C(C(N[C@@H](C2=CC=C(OC(F)(F)F)C(F)=C2)C3=NC=CC=C3F)=O)C=C1
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| InChi Key |
QEBYISWYMFIXOZ-INIZCTEOSA-N
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| InChi Code |
InChI=1S/C20H12F5N3O4/c21-12-2-1-7-26-17(12)16(10-4-6-15(13(22)8-10)32-20(23,24)25)28-18(29)14-5-3-11(9-27-14)19(30)31/h1-9,16H,(H,28,29)(H,30,31)/t16-/m0/s1
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| Chemical Name |
(S)-6-(((3-fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic acid
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| Synonyms |
AMG-333; AMG 333; AMG333
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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 : ≥ 125 mg/mL (~275.74 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2059 mL | 11.0297 mL | 22.0595 mL | |
| 5 mM | 0.4412 mL | 2.2059 mL | 4.4119 mL | |
| 10 mM | 0.2206 mL | 1.1030 mL | 2.2059 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.
Products are for research use only; We do not sell to patients
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