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Fasudil dihydrochloride
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Catalog No. T61382Cas No. 203911-27-7
Alias HA-1077 dihydrochloride, HA1077 dihydrochloride, AT-877 dihydrochloride, AT877 dihydrochloride
Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. Fasudil dihydrochloride exhibits inhibitory effects on protein kinases including ROCK1 (Ki = 0.33 μM), ROCK2 (IC50 = 0.158 μM), PKA (IC50 = 4.58 μM), PKC (IC50 = 12.30 μM), and PKG (IC50 = 1.650 μM), while also acting as a potent Ca2+ channel blocker and vasodilator, providing a multifunctional pharmacological tool for vascular, cardiovascular, and cellular signaling research.
Fasudil dihydrochloride
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Purity: 99.86%
Catalog No. T61382Alias HA-1077 dihydrochloride, HA1077 dihydrochloride, AT-877 dihydrochloride, AT877 dihydrochlorideCas No. 203911-27-7
Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. Fasudil dihydrochloride exhibits inhibitory effects on protein kinases including ROCK1 (Ki = 0.33 μM), ROCK2 (IC50 = 0.158 μM), PKA (IC50 = 4.58 μM), PKC (IC50 = 12.30 μM), and PKG (IC50 = 1.650 μM), while also acting as a potent Ca2+ channel blocker and vasodilator, providing a multifunctional pharmacological tool for vascular, cardiovascular, and cellular signaling research.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | $30 | - | In Stock | |
| 25 mg | $48 | - | In Stock | |
| 50 mg | $79 | - | In Stock | |
| 100 mg | $123 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.86%
Appearance:Solid
Color:White
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| Description | Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. Fasudil dihydrochloride exhibits inhibitory effects on protein kinases including ROCK1 (Ki = 0.33 μM), ROCK2 (IC50 = 0.158 μM), PKA (IC50 = 4.58 μM), PKC (IC50 = 12.30 μM), and PKG (IC50 = 1.650 μM), while also acting as a potent Ca2+ channel blocker and vasodilator, providing a multifunctional pharmacological tool for vascular, cardiovascular, and cellular signaling research. |
| Targets&IC50 | ROCK2:0.158 μM, ROCK1 (p160ROCK):0.33 μM (Ki), PKG:1.65 μM, PKC:12.3 μM, PKA:4.58 μM |
| In vitro | Fasudil dihydrochloride (100 μM) can inhibit cell spreading, stress fiber formation, and α-SMA expression in rat hepatic stellate cells (HSCs) and human HSC-derived TWNT-4 cells, while also significantly suppressing the proliferation of these two cell types [4]. Fasudil dihydrochloride (50–100 μM) can inhibit lysophosphatidic acid (LPA)-induced phosphorylation levels of ERK1/2, JNK, and p38 in rat hepatic stellate cells and human HSC-derived TWNT-4 cells [4]. Fasudil dihydrochloride (25–100 μM, 24 h) can suppress the transcription of collagen and tissue inhibitor of metalloproteinases (TIMP), and simultaneously promote the transcription of matrix metalloproteinase-1 (MMP-1) in human HSC-derived TWNT-4 cells [4]. |
| In vivo | Fasudil dihydrochloride (10 mg/kg, i.v., administered 1 hour before surgery) exhibits protective effects on the cardiovascular system under ischemic injury conditions, reduces the activation level of JNK, and attenuates the mitochondrial-nuclear translocation of AIF [5]. Fasudil dihydrochloride (50 mg/kg/day, i.p.) can suppress acute and recurrent EAE induced by proteolipid protein PLP p139-151, inhibit lymphocyte proliferation, downregulate the expression of IL-17, and significantly reduce the IFN-γ/IL-4 ratio [6]. Fasudil dihydrochloride (100 mg/kg/day, p.o.) significantly decreases the incidence and pathological scores of EAE in SJL/J mice, while alleviating inflammatory responses, demyelination, axonal loss in spinal cord tissues, and reducing the accumulation of APP-positive signals in the spinal cord [6]. |
| Synonyms | HA-1077 dihydrochloride, HA1077 dihydrochloride, AT-877 dihydrochloride, AT877 dihydrochloride |
| Molecular Weight | 364.29 |
| Formula | C14H19Cl2N3O2S |
| Cas No. | 203911-27-7 |
| Smiles | O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O.Cl.Cl |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | H2O: ≥ 80 mg/mL, Sonication is recommeded. DMSO: 16 mg/mL (43.92 mM), Sonication is recommeded. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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