| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
Z62954982 (5-100 μM; 4-hour duration) exhibits a concentration-dependent reduction in intracellular Rac1-GTP levels, demonstrating the most inhibitory effect on Human SMCs with an IC50 of 12.2 μM[1]. In cultured SMCs, Z62954982 (25 μM; 4 hours) has the most inhibitory effect (86.0%) and dramatically lowers the ratio Rac1-GTP/Rac1[1]. In both HDMEC and HUVEC monolayers, Z62954982 (10-100 μM; 72 hours) results in a concentration-dependent reduction in transendothelial electrical resistance (TER)[2].
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| ln Vivo |
Z62954982 (intraperitoneal injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks) has been shown to reduce p38 phosphorylation and released IL-6 in PASMCs in response to hypoxia in both bcr-/- and abr-/-mice[3]. It also shows no overt toxicity.
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| Animal Protocol |
Animal/Disease Models: Male bcr-/-, abr-/- and wt mice (8 to 10weeks old littermates) are exposed to hypoxia (10% O2) or normoxia (21% O2) for 3 weeks[3]
Doses: 10 mg/kg or 20 mg/kg Route of Administration: intraperitoneal (ip) injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks Experimental Results: Promoted phosphorylation of p38 MAPK and increased IL-6 in Hypoxia in mice. |
| References |
[1]. Nicola Ferri,et al. Virtual Screening Approach for the Identification of New Rac1 Inhibitors. J Med Chem. 2009 Jul 23;52(14):4087-90.
[2]. Xun E Zhang, et al. Activation of RhoA, but Not Rac1, Mediates Early Stages of S1P-Induced Endothelial Barrier Enhancement. PLoS One. 2016 May 17;11(5):e0155490. [3]. Min Yu, et al. Lack of BCR and Abr Promotes Hypoxia-Induced Pulmonary Hypertension in Mice. PLoS One |
| Molecular Formula |
C20H21N3O5S
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|---|---|
| Molecular Weight |
415.46
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| CAS # |
1090893-12-1
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| SMILES |
O1[C@H](CO)[C@H]([C@H]([C@@H]1N1C=NC2C(N)=NC(C#CCCCCCC)=NC1=2)O)O
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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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4070 mL | 12.0349 mL | 24.0697 mL | |
| 5 mM | 0.4814 mL | 2.4070 mL | 4.8139 mL | |
| 10 mM | 0.2407 mL | 1.2035 mL | 2.4070 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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