| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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BDP5290 is a novel, potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively. 3 μM. BDP5290 totally prevents phosphorylation of the myosin II light chain (MLC) caused by MRCKβ, but not that of ROCK1 or ROCK2. At higher concentrations, MLC phosphorylation (pMLC) is reduced by BDP5290 to undetectable levels.
| Targets |
ROCK1 (IC50 = 5 nM); ROCK2 (IC50 = 50 nM); MRCKα (IC50 = 10 nM); MRCKβ (IC50 = 100 nM)
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| ln Vitro |
BDP5290's Ki for MRCKα is 10 nM, marginally greater than MRCKβ's Ki of 4 nM. The phosphorylation of myosin II light chain (MLC) caused by MRCKβ is entirely inhibited by 3 μM BDP5290, but not by ROCK1 or ROCK2. Increased BDP5290 concentrations cause MLC phosphorylation (pMLC) to drop to undetectable levels. At every tested concentration, beginning at 0.1 μM, BDP5290 decreases MDA-MB-231 invasion, reaching nearly complete inhibition at 10 μM. Cell viability is marginally decreased with an EC50 value >10 μM after 24 hours in the presence of BDP5290. At 1 μM BDP5290, which has no effect on cell viability, wound closure is inhibited by more than 60%[2].
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| References |
| Molecular Formula |
C17H18CLN7O
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|---|---|
| Molecular Weight |
371.824120998383
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| Exact Mass |
407.1
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| Elemental Analysis |
C, 50.01; H, 4.69; Cl, 17.37; N, 24.01; O, 3.92
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| CAS # |
1817698-21-7
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| Related CAS # |
1817698-21-7
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| PubChem CID |
85325326
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| Appearance |
White to off-white solid powder
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| LogP |
1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
490
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BPVZKUXLOLRECL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18ClN7O/c18-12-10-25(11-4-7-19-8-5-11)24-15(12)17(26)22-14-9-21-23-16(14)13-3-1-2-6-20-13/h1-3,6,9-11,19H,4-5,7-8H2,(H,21,23)(H,22,26)
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| Chemical Name |
4-chloro-1-piperidin-4-yl-N-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyrazole-3-carboxamide
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| Synonyms |
BDP00005290; BDP-5290; BDP5290 HCl; BDP 5290
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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 |
| 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) |
DMSO: ~12.5 mg/mL (~33.6 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6895 mL | 13.4474 mL | 26.8947 mL | |
| 5 mM | 0.5379 mL | 2.6895 mL | 5.3789 mL | |
| 10 mM | 0.2689 mL | 1.3447 mL | 2.6895 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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