SKA-31 structure
|
Common Name | SKA-31 | ||
---|---|---|---|---|
CAS Number | 40172-65-4 | Molecular Weight | 200.26 | |
Density | 1.403g/cm3 | Boiling Point | 417.1ºC at 760 mmHg | |
Molecular Formula | C11H8N2S | Melting Point | 184-188ºC | |
MSDS | Chinese USA | Flash Point | 206.1ºC | |
Symbol |
GHS07 |
Signal Word | Warning |
Use of SKA-31SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure[1]. |
Name | benzo[e][1,3]benzothiazol-2-amine |
---|---|
Synonym | More Synonyms |
Description | SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure[1]. |
---|---|
Related Catalog | |
Target |
EC50: 2.9 μM (KCa2.1), 1.9 μM (KCa2.2), 2.9 μM (KCa2.3), 260 nM (KCa3.1)[1] |
In Vitro | SKA-31 activates KCa2/3 Channels more potently than Riluzole, and is more selective over other Ion channels[1]. SKA-31 reduces cell viability with IC50s of 5.3 μM , 46.9 μm in HCT-116 cells and HCT-8 cells, respectively[2]. SKA-31 (5.3 μM; 0-96 hours) reduces HCT-116 cells proliferation when added at time zero at IC50 value[2]. SKA-31 triggers apoptosis in HCT-116 cells at 5 μM, and the effect is smaller in HCT-8 cells at 45 μM[2]. SKA-31 increases the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines at 5 μM and 45 μM, respectively[2]. SKA-31 further activates Caspase 3 and reduces Akt phosphorylation induced by Cisplatin[2]. SKA-31 has a synergic effect with Cisplatin also on the inhibition of HCT-116 cell proliferation[2]. Cell Viability Assay[2] Cell Line: HCT-116 cells, HCT-8 cells Concentration: Incubation Time: 24 hours Result: Reduced cell viability with IC50s of 5.3 μM , 46.9 μm in HCT-116 and HCT-8, respectively. Cell Proliferation Assay[2] Cell Line: HCT-116 cells Concentration: 5.3 μM Incubation Time: 0-96 hours Result: Reduced HCT-116 cells proliferation when added at time zero at IC50S value. Apoptosis Analysis[2] Cell Line: HCT-116 cells, HCT-8 cells Concentration: 5 μM (HCT-116 cells), 45 μM (HCT-8 cells) Incubation Time: 24 hours Result: Triggered apoptosis in HCT-116 cells, and the effect was smaller in HCT-8 cells. Cell Cycle Analysis[2] Cell Line: HCT-116cells, HCT-8 cells Concentration: 5 μM (HCT-116), 45 μM (HCT-8) Incubation Time: 24 hours Result: Increased the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines. Western Blot Analysis[2] Cell Line: HCT-116 cells Concentration: Incubation Time: 24 hours Result: Further activated Caspase 3 and reduced Akt phosphorylation when co-treatment with Cisplatin in HCT-116 cells. |
In Vivo | SKA-31 Is not acutely toxic and has good pharmacokinetic properties[1]. SKA-31 potentiates native KCa3.1 and KCa2.3 in murine carotid endothelium with EC50 values of 225 nM and 1.6 μM for KCa3.1 and KCa2.3, respectively[1]. SKA-31 stimulates KCa3.1 and KCa2.3 in vascular endothelial cells and increases acetylcholine-induced endothelium-derived hyperpolarizing factor (EDHF) -mediated vasodilation[1]. SKA-31 potentiates EDHF-type vasodilations and lowers blood pressure in mice. Injections of SKA-31 (1-30 mg/kg; i.p.) lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-)[1]. Animal Model: 16-25 weeks mice[1] Dosage: 1 mg/kg, 10 mg/kg, and 30 mg/kg Administration: Intraperitoneal injection Result: Lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-). |
References |
Density | 1.403g/cm3 |
---|---|
Boiling Point | 417.1ºC at 760 mmHg |
Melting Point | 184-188ºC |
Molecular Formula | C11H8N2S |
Molecular Weight | 200.26 |
Flash Point | 206.1ºC |
Exact Mass | 200.04100 |
PSA | 67.15000 |
LogP | 3.61290 |
Index of Refraction | 1.83 |
Storage condition | Store at +4°C |
Symbol |
GHS07 |
---|---|
Signal Word | Warning |
Hazard Statements | H302-H319 |
Precautionary Statements | P305 + P351 + P338 |
Hazard Codes | Xn |
Risk Phrases | 20/21/22-36/37/38 |
Safety Phrases | 22-36/37/39 |
RIDADR | NONH for all modes of transport |
HS Code | 2934999090 |
~89% SKA-31 CAS#:40172-65-4 |
Literature: Zhao, Jinwu; Huang, Huawen; Wu, Wanqing; Chen, Huoji; Jiang, Huanfeng Organic Letters, 2013 , vol. 15, # 11 p. 2604 - 2607 |
~80% SKA-31 CAS#:40172-65-4 |
Literature: Liu; Lee; Shih; Chen; Tao Archiv der Pharmazie, 1982 , vol. 315, # 10 p. 872 - 877 |
~61% SKA-31 CAS#:40172-65-4 |
Literature: Moradi Rufchahi; Yousefi, Hessamoddin; Mohammadinia, Mojgan Journal of Molecular Liquids, 2013 , vol. 188, p. 173 - 177 |
~% SKA-31 CAS#:40172-65-4 |
Literature: Ubaldini; Fiorenza Gazzetta Chimica Italiana, 1946 , vol. 76, p. 215,221 |
~% SKA-31 CAS#:40172-65-4 |
Literature: Freund Chemische Berichte, 1891 , vol. 24, p. 4187 |
~% SKA-31 CAS#:40172-65-4 |
Literature: Kajino; Mizuno; Tawada; Shibouta; Nishikawa; Meguro Chemical and Pharmaceutical Bulletin, 1991 , vol. 39, # 11 p. 2888 - 2895 |
~% SKA-31 CAS#:40172-65-4 |
Literature: Gorelik,M.V.; Lomzakova,V.I. Zhurnal Organicheskoi Khimii, 1978 , vol. 14, # 5 p. 1051 - 1055,981 - 985 |
Precursor 7 | |
---|---|
DownStream 5 | |
HS Code | 2934999090 |
---|---|
Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
F1386-0401 |
naphtho[1,2-d]thiazol-2-amine |
MFCD00051329 |
2-Aminonaphthiazole |
EINECS 254-822-1 |
2-amminonafto<1,2-a>tiazolo |
2-Aminonaphtol<1,2-d>thiazole |
Naphtho[1,2-d]thiazol-2-ylamine |
2-Aminonaphtho<thiazol |