JTV-519 hemifumarate
Based on 1 Customer Validation
JTV-519 hemifumarate (K201 hemifumarate) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
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- Purity: 99.74%
- CAS No.: 1435938-25-2
- 화학식: C25H32N2O2S.1/2C4H4O4
- 분자량:482.64
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
JTV-519 (K201) inhibits inward Ca2+ movement into large unilamellar vesicles (LUV) caused by annexin V in a dose-dependent manner. In the presence of 50 nM annexin V and 400 μM Ca2+, 3 μM JTV-519 shows significant inhibition of Ca2+ movement due to annexin V, and 50% inhibition is achieved at 25 μM K201[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild type male C57BL/6 mice weighing 18-22g with polymicrobial sepsis produced by cecal ligation and puncture (CLP) [3]
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Dosage:0.5 mg/kg/h
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Administration:Applied intraperitoneally 2 h before the surgery
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Result:Improved cardiac function, where the EF and FS were significantly increased.
Chemical Information
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CAS No. 1435938-25-2
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Appearance Solid
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분자량 482.64
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화학식 C25H32N2O2S.1/2C4H4O4
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Color White to off-white
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SMILES
O=C(N1CCSC2=CC=C(OC)C=C2C1)CCN3CCC(CC4=CC=CC=C4)CC3.O=C(O)/C=C/C(O)=O.[1/2]
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Synonyms
K201 hemifumarate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (207.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Darcy YL, et al. K201 (JTV519) is a Ca2+-Dependent Blocker of SERCA and a Partial Agonist of Ryanodine Receptors in Striated Muscle. Mol Pharmacol. 2016 Aug;90(2):106-15. [Content Brief]
[2]. Kaneko N, et al. Inhibition of annexin V-dependent Ca2+ movement in large unilamellar vesicles by K201, a new 1,4-benzothiazepine derivative. Biochim Biophys Acta. 1997 Nov 13;1330(1):1-7. [Content Brief]
[3]. Yang J, et al. Toll-like receptor 4-induced ryanodine receptor 2 oxidation and sarcoplasmic reticulum Ca2+ leakage promote cardiac contractile dysfunction in sepsis. J Biol Chem. 2018 Jan 19;293(3):794-807. [Content Brief]
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 | 2.0719 mL | 10.3597 mL | 20.7194 mL | 51.7984 mL |
| 5 mM | 0.4144 mL | 2.0719 mL | 4.1439 mL | 10.3597 mL | |
| 10 mM | 0.2072 mL | 1.0360 mL | 2.0719 mL | 5.1798 mL | |
| 15 mM | 0.1381 mL | 0.6906 mL | 1.3813 mL | 3.4532 mL | |
| 20 mM | 0.1036 mL | 0.5180 mL | 1.0360 mL | 2.5899 mL | |
| 25 mM | 0.0829 mL | 0.4144 mL | 0.8288 mL | 2.0719 mL | |
| 30 mM | 0.0691 mL | 0.3453 mL | 0.6906 mL | 1.7266 mL | |
| 40 mM | 0.0518 mL | 0.2590 mL | 0.5180 mL | 1.2950 mL | |
| 50 mM | 0.0414 mL | 0.2072 mL | 0.4144 mL | 1.0360 mL | |
| 60 mM | 0.0345 mL | 0.1727 mL | 0.3453 mL | 0.8633 mL | |
| 80 mM | 0.0259 mL | 0.1295 mL | 0.2590 mL | 0.6475 mL | |
| 100 mM | 0.0207 mL | 0.1036 mL | 0.2072 mL | 0.5180 mL |
JTV-519 hemifumarate Related Classifications
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