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Purity: ≥98%
ASK1-IN-1 is a potent inhibitor of the apoptosis signal regulating kinase 1 (ASK1) inhibitor (Compound 4 from patent WO2016025474A1). In an in vivo pulmonary hypertension (PH) model, it reduces right ventricular (RV) hypertrophy and pulmonary arterial pressure dose-dependently. The hallmarks of pulmonary vascular disease, including but not limited to decreased pulmonary vascular resistance (PVR), improved pulmonary pressure, decreased pulmonary vascular remodeling, improved vascular function, decreased maladaptive RV hypertrophy, and improved RV function, can all be lessened by inhibiting ASKl. The pathological alterations linked to PH may also be slowed, avoided, and/or reversed by inhibiting ASKl signaling.
| Targets |
ASK1 (IC50 = 2.87 nM)
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| ln Vitro |
ASK1-IN-1 is a potent inhibitor of the apoptosis signal regulating kinase 1 (ASK1) inhibitor (Compound 4 from patent WO2016025474A1). In an in vivo pulmonary hypertension (PH) model, it reduces right ventricular (RV) hypertrophy and pulmonary arterial pressure in a dose-dependent manner. The hallmarks of pulmonary vascular disease, such as reduced pulmonary vascular resistance (PVR), improved pulmonary pressure, decreased pulmonary vascular remodeling, improved vascular function, decreased maladaptive RV hypertrophy, and improved RV function, can all be lessened by inhibiting ASKl. The pathological changes linked to PH may also be slowed, avoided, and/or reversed by inhibiting ASKl signaling.
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| ln Vivo |
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| Enzyme Assay |
ASKl inhibition improves vascular function and decreases the signs and symptoms of pulmonary vascular disease, such as pulmonary vascular resistance (PVR), pulmonary pressure, remodeling of the pulmonary arteries, maladaptive RV hypertrophy, and RV function. The pathological changes linked to PH may be slowed, avoided, or even reversed by inhibiting ASKl signaling. Both of the ASK1-IN-1 doses—0.1+0.05 for 0.1% and 0.1±0.1 ng/mL for 0.2%—reduce plasma levels of B-type natriuretic peptide (BNP). ASK1-IN-1 treatment reduced the number of completely muscularized arterioles in Su/Hx rats by 35.6% or 32.6%, respectively.
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| References |
| Molecular Formula |
C₂₃H₂₁N₇O
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| Molecular Weight |
411.46
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| Exact Mass |
411.18
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| Elemental Analysis |
C, 67.14; H, 5.14; N, 23.83; O, 3.89
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| CAS # |
1262041-49-5
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1CC1C2=CN(C=N2)C3=CC(=NC=C3)C(=O)NC4=CC=CC(=C4)C5=NN=CN5C6CC6
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| InChi Key |
ZGCMQKWOUIMBEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H21N7O/c31-23(20-11-19(8-9-24-20)29-12-21(25-13-29)15-4-5-15)27-17-3-1-2-16(10-17)22-28-26-14-30(22)18-6-7-18/h1-3,8-15,18H,4-7H2,(H,27,31)
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| Chemical Name |
4-(4-cyclopropylimidazol-1-yl)-N-[3-(4-cyclopropyl-1,2,4-triazol-3-yl)phenyl]pyridine-2-carboxamide
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.08 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 25.0 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: ≥ 2.5 mg/mL (6.08 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 25.0 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: ≥ 2.5 mg/mL (6.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4304 mL | 12.1518 mL | 24.3037 mL | |
| 5 mM | 0.4861 mL | 2.4304 mL | 4.8607 mL | |
| 10 mM | 0.2430 mL | 1.2152 mL | 2.4304 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.
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