| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Belumosudil (formerly known as KD-025, ROCK inhibitor, and SLx-2119; trade name Rezurock) is a novel, potent, orally bioavailable, and selective small molecule ROCK2 inhibitor that has been approved by FDA in July 2021 for the treatment of chronic graft versus host disease (cGvHD). It inhibits ROCK2 with IC50 and Ki of 60 nM and 41 nM, respectively. In smooth muscle cells isolated from human intestine with radiation-induced fibrosis (RE-SMC), SLx-2119 reduced mRNA level of CTGF. Over-expression of which is associated with fibrotic diseases. While, in SMC isolated from normal human intestine (N-SMC), SLx-2119 didn't change CTGF mRNA level.
| ln Vitro |
Tsp-1 and CTGF mRNA levels in PASMC are significantly down-regulated by belumosudil (SLx-2119; 40 µM). Compared to the other arrays, the microarray hybridized with aRNA from HMVEC treated with belumosudil has a 5-times greater background[1].
|
||
|---|---|---|---|
| ln Vivo |
After temporary middle cerebral artery blockage, belumosudil (KD-025; 100, 200, or 300 mg/kg, ip) dose-dependently decreases the infarct volume. Belumosudil works just as well in old, diabetic, or female mice as it does in healthy adult male mice[2].
|
||
| Animal Protocol |
|
||
| References |
[1]. Boerma, M., et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase. Blood Coagul Fibrinolysis. 2008 Oct;19(7):709-18.
[2]. Lee, J.H., et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14 |
| Molecular Formula |
C26H24N6O2
|
|---|---|
| Molecular Weight |
452.51
|
| CAS # |
911417-87-3
|
| Related CAS # |
Belumosudil mesylate;2109704-99-4
|
| SMILES |
O=C(NC(C)C)COC1=CC=CC(C2=NC(NC3=CC4=C(NN=C4)C=C3)=C5C=CC=CC5=N2)=C1
|
| Chemical Name |
2-[3-[4-(1H-indazol-5-ylamino)-2-quinazolinyl]phenoxy]-N-(1-methylethyl)-acetamide
|
| Synonyms |
Belumosudil; KD-025; SLx-2119; KD025; SLx2119; KD 025; SLx 2119; ROCK inhibitor;
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 20.8 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: 3.33 mg/mL (7.36 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2099 mL | 11.0495 mL | 22.0990 mL | |
| 5 mM | 0.4420 mL | 2.2099 mL | 4.4198 mL | |
| 10 mM | 0.2210 mL | 1.1049 mL | 2.2099 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
