Size | Price | Stock | Qty |
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1mg |
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Other Sizes |
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Targets |
PKCα 9.3 nM (IC50) PKC-βI 28 nM (IC50) PKC-βII 30 nM (IC50) PKCγ 36.5 nM (IC50) PKCε 108.3 nM (IC50) G protein-coupled receptor kinase 5 (GRK5)
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ln Vitro |
(S)-Ro 32-0432 suppresses the release of interleukin-2 (IL-2) and the expression of IL-2 receptors in peripheral human T-cells stimulated with phorbol ester in combination with phytohemagglutin or anti-CD3. However, it has no effect on the proliferation of IL-2-induced cells that have already been stimulated to express IL-2 receptors. The influenza peptide antigen HA 307-319-specific human T-cell clone (HA27) is also blocked by (S)-Ro 32-0432 from proliferating after being exposed to antigen-pulsed autologous presentation cells. HA27 proliferation is inhibited by (S)-Ro 32-0432, with an IC50 of 0.15 μM[1].
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ln Vivo |
Treatment with (S)-Ro 32-0432 (10–50 mg/kg; oral dose; once; female AHH/R rats) prevents edema produced by phorbol ester in rats later on, indicating the compound's systemic effectiveness in suppressing PKC-driven reactions. Ro 32-0432 also inhibits the induction of more physiologically driven T-cell responses, such as host versus graft responses and subsequent paw edema in adjuvant-induced arthritis[1].
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Animal Protocol |
Animal/Disease Models: Female AHH/R rats (200-250 g) induced with phorbol ester[1]
Doses: 10 mg/kg, 30 mg/kg, 50 mg/kg Route of Administration: Oral administration; once Experimental Results: Inhibited subsequent phorbol ester-induced edema in rats. |
References |
[1]. A M Birchall, et al. Ro 32-0432, a Selective and Orally Active Inhibitor of Protein Kinase C Prevents T-cell Activation. J Pharmacol Exp Ther. 1994 Feb;268(2):922-9.
[2]. Thakur Gurjeet Singh, et al. Ro 32-0432 Attenuates Mecamylamine-Precipitated Nicotine Withdrawal Syndrome in Mice. Naunyn Schmiedebergs Arch Pharmacol. 2013 Mar;386(3):197-204. |
Molecular Formula |
C28H29CLN4O2
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Molecular Weight |
489.01
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CAS # |
1781828-85-0
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SMILES |
Cl.O=C1C(=C(C(N1)=O)C1=CN(C)C2C=CC=CC1=2)C1C2C=CC=CC=2N2CC[C@H](CN(C)C)CC2=1
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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 | 2.0449 mL | 10.2247 mL | 20.4495 mL | |
5 mM | 0.4090 mL | 2.0449 mL | 4.0899 mL | |
10 mM | 0.2045 mL | 1.0225 mL | 2.0449 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.