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| ln Vitro |
In the murine mixed lymphocyte response (MLR) experiments, tautomycetin (100 ng/ml–10 μg/ml; 48 hours) inhibits T cell growth. TMC has a 100-fold greater amount of MLR inhibition than CsA, and its IC50 is 7.8 nM[1]. Tautomycetin (1 μg/ml) has immunosuppressive properties that prevent T cell proliferation by preventing human primary T cells from secreting IL-2[1]. /ml; pretreated for 5 hours) stimulates T cells with immobilized OKT3 mAb, and it phosphorylates tyrosine residues on a number of particular cellular proteins in a manner that is dependent on both time and dose[1]. In the Jurkat TAg cell line, tautomycetin (1 μg/ml; 5 hours) substantially and dose-dependently suppresses the phosphorylation of Akt and BAD[1].
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| ln Vivo |
Tautomycetin (intraperitoneal injection; 0.03 mg/kg–5 mg/kg; 30 days) suppresses the immune system in vivo after the transplantation of a cardiac allograft. Furthermore, no appreciable liver or renal damage was observed in rats given TMC at doses up to 5 mg/kg for 30 days, according to a biochemical study of GOP, GTP, glucose, and creatine levels in blood[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Human primary B cells Tested Concentrations: 1 μg/ml Incubation Duration: Pretreated for 5 hrs (hours), and then stimulated with immobilized OKT3 mAb (10 μg/ml) for 0, 5, 10 miuntes Experimental Results: Blocked tyrosine phosphorylation of intracellular signal mediators. Apoptosis Analysis[1] Cell Types: Jurkat T cells Tested Concentrations: 1 μg/ml Incubation Duration: 5 hour Experimental Results: Induces cell apoptosis. |
| Animal Protocol |
Animal/Disease Models: Rat[2]
Doses: 0.03 mg/kg, 0.5 mg/kg, 5 mg/kg; 30 days Route of Administration: intraperitoneal (ip)injection Experimental Results: demonstrated immunosuppressive effects in vivo |
| References |
[1]. S Mitsuhashi, et al. Tautomycetin is a novel and specific inhibitor of serine/threonine protein phosphatase type 1, PP1. Biochem Biophys Res Commun. 2001 Sep 21;287(2):328-31.
[2]. Jae-Hyuck Shim, et al. Immunosuppressive effects of tautomycetin in vivo and in vitro via T cell-specific apoptosis induction. Proc Natl Acad Sci U S A. 2002 Aug 6;99(16):10617-22. |
| Molecular Formula |
C33H50O10
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|---|---|
| Molecular Weight |
606.74
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| CAS # |
119757-73-2
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| SMILES |
O([H])C([H])(C([H])(C([H])([H])[H])C(C([H])([H])C([H])(C([H])(C([H])([H])[H])C([H])(C([H])([H])[H])OC(C([H])([H])C([H])(C1C(=O)OC(C=1C([H])([H])[H])=O)O[H])=O)O[H])=O)C([H])([H])C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C(/C(/[H])=C(/C([H])=C([H])[H])\C([H])([H])C([H])([H])[H])=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 | 1.6482 mL | 8.2408 mL | 16.4815 mL | |
| 5 mM | 0.3296 mL | 1.6482 mL | 3.2963 mL | |
| 10 mM | 0.1648 mL | 0.8241 mL | 1.6482 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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