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Antiviral API
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Fasudil-hydrochloride-semihydrate
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| Category | Human immunodeficiency Virus (HIV) |
| CAS | 186694-02-0 |
| Description | Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca2+ channel antagonist and vasodilator. |
Product Information
| Molecular Weight | 673.68 |
| Molecular Formula | C14H18ClN3O2.5S |
| Boiling Point | 506.2ºC at 760 mmHg |
| Melting Point | 222 °C(dec.) |
| Flash Point | 259.9ºC |
| Purity | ≥98% (HPLC) |
| Solubility | In vitro: 10 mM in DMSO |
| Appearance | Solid powder |
| Storage | Store at -20°C |
| In Vitro | Fasudil hydrochloride semihydrate (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells. Fasudil hydrochloride semihydrate (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells. Fasudil hydrochloride semihydrate (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells. |
| In Vivo | Fasudil hydrochloride semihydrate (10 mg/kg; i.v.; 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. Fasudil hydrochloride semihydrate (50 mg/kg/d; i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio. Fasudil hydrochloride semihydrate(100 mg/kg/d; p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice. |
| PSA | 70.68000 |
| Target | ROCK; Calcium Channel; Autophagy; HIV; PKA; PKC |
