| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
SB-7720770 2HCl targets Rho kinase (ROCK), specifically the ROCK1 and ROCK2 isoforms. It is a potent inhibitor with IC₅₀ values of 5.6 nM for ROCK1 and 6 nM for ROCK2. ROCK is a key regulator of the actin cytoskeleton and is involved in various cellular processes including smooth muscle contraction and cell migration.
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| ln Vitro |
In vitro, SB-7720770 2HCl demonstrates potent inhibition of ROCK1 and ROCK2 with IC₅₀ values of 5.6 nM and 6 nM, respectively. The compound's activity is confirmed in kinase assays using recombinant ROCK enzymes. It shows high selectivity for ROCK over other kinases. The inhibitory activity is measured by the phosphorylation of ROCK substrates.
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| ln Vivo |
In vivo, oral administration of SB-772077-B produced a profound dose-dependent reduction of systemic blood pressure in spontaneously hypertensive rats. At doses of 1, 3, and 30 mg/kg, it induced reductions in blood pressure of approximately 10, 20, and 50 mm Hg. It also dramatically lowered blood pressure in DOCA salt-induced hypertensive rats.
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| Enzyme Assay |
The in vitro enzyme assay for SB-7720770 2HCl involves measuring the inhibition of ROCK1 and ROCK2 kinase activity. Recombinant ROCK enzymes are incubated with the compound and a peptide substrate in the presence of ATP. The phosphorylation of the substrate is quantified using methods such as radiometric detection or fluorescence. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based assays are performed using cell lines that express ROCK, such as vascular smooth muscle cells. Cells are treated with SB-7720770 2HCl, and ROCK activity is measured by assessing the phosphorylation of downstream targets such as myosin light chain (MLC) or cofilin. Cell proliferation, migration, and morphological changes are also assessed.
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| Animal Protocol |
In vivo animal experiments for SB-7720770 2HCl have been conducted in spontaneously hypertensive rats and DOCA salt-induced hypertensive rats. Animals are administered the compound orally, and blood pressure is measured using telemetry or tail-cuff methods. Dose-response relationships are established. The compound's effects on heart rate and other cardiovascular parameters are also evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SB-7720770 2HCl have been characterized in preclinical species. It is orally bioavailable and achieves sufficient plasma concentrations to exert its pharmacological effects. Detailed PK parameters such as half-life, clearance, volume of distribution, and oral bioavailability are determined from plasma concentration-time profiles following intravenous and oral dosing.
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| Toxicity/Toxicokinetics |
Toxicological data for SB-7720770 2HCl are limited as it is primarily a research tool compound. In standard preclinical safety assessments, it would be evaluated for potential off-target effects and general toxicity in rodent and non-rodent species. The compound is intended for research use only and not for therapeutic use in humans.
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| References | |
| Additional Infomation |
SB-7720770 2HCl is a novel aminofurazan-based ROCK inhibitor that has demonstrated profound vasodilatory and antihypertensive effects in animal models. It represents a promising tool for studying the role of ROCK in cardiovascular diseases and other chronic conditions. It has not been approved for clinical use and remains an investigational research compound.
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| Molecular Formula |
C15H20CL2N8O2
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|---|---|
| Molecular Weight |
415.27769947052
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| Exact Mass |
414.109
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| CAS # |
607373-46-6
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| PubChem CID |
69157798
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| Appearance |
White to off-white solid powder
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| LogP |
3.08
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
508
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCN1C2=C(C=NC=C2C(=O)N3CC[C@@H](C3)N)N=C1C4=NON=C4N.Cl.Cl
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| InChi Key |
HSROPTGRSYJPJY-JZGIKJSDSA-N
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| InChi Code |
InChI=1S/C15H18N8O2.2ClH/c1-2-23-12-9(15(24)22-4-3-8(16)7-22)5-18-6-10(12)19-14(23)11-13(17)21-25-20-11;;/h5-6,8H,2-4,7,16H2,1H3,(H2,17,21);2*1H/t8-;;/m0../s1
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| Chemical Name |
4-(7-{[(3S)-3-Amino-1-pyrrolidinyl]carbonyl}-1-ethyl-1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine dihydrochloride
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| Synonyms |
SB-7720770; SB 7720770; SB7720770; SB-7720770 2HCl; SB 7720770 2HCl; SB7720770 2HCl; SB-7720770 dihydrochloride; SB 7720770 dihydrochloride; SB7720770 dihydrochloride;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~240.80 mM)
DMSO : ~38.33 mg/mL (~92.30 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.83 mg/mL (9.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 38.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3.83 mg/mL (9.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 38.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3.83 mg/mL (9.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (60.20 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4080 mL | 12.0401 mL | 24.0801 mL | |
| 5 mM | 0.4816 mL | 2.4080 mL | 4.8160 mL | |
| 10 mM | 0.2408 mL | 1.2040 mL | 2.4080 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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