| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Dynamin-related protein 1 (Drp1), specifically the GTPase domain of Drp1, binding via hydrogen bonds to Gln34 and Asp218.
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| ln Vitro |
DRP1i27 (0-50 μM) dihydrochloride binds directly to human Drp1 and suppresses its GTPase activity [1]. In a Drp1-dependent way, DRP1i27 (0-50 μM) dihydrochloride expands the mitochondrial cellular network in human and mouse fibroblasts [1]. The SPR assay yields a binding affinity of 286 μM for DRP1i27 dihydrochloride, while the MST assay yields a KD value of 190 μM [1].
DRP1i27 dihydrochloride binds directly to Drp1 (KD=190 microM by MST, 286 microM by SPR) and inhibits its GTPase activity at 0-50 microM; increases mitochondrial network connectivity in human and mouse fibroblasts in a Drp1-dependent manner. |
| ln Vivo |
Targets Drp1-mediated mitochondrial fission in cell line models; protects against simulated ischemia-reperfusion injury; promotes mitochondrial fusion over fission, potentially applicable in neurodegenerative and cardiovascular disease models.
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| Enzyme Assay |
Binding affinity assessed by surface plasmon resonance (SPR) yielding 286 microM and microscale thermophoresis (MST) yielding KD value of 190 microM for Drp1 binding.
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| Cell Assay |
Human and mouse fibroblasts are treated with DRP1i27 (0-50 microM) for 24-72 h; mitochondrial morphology is visualized by MitoTracker staining or confocal microscopy; Drp1 GTPase activity is measured via malachite green phosphate assay.
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| Animal Protocol |
Standard Drp1 inhibitor in vivo protocol: mice with myocardial or cerebral ischemia are administered DRP1i27 (5-10 mg/kg, IV or IP) before reperfusion; infarct size and mitochondrial morphology are assessed.
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| ADME/Pharmacokinetics |
Limited PK data available; as a small molecule GTPase inhibitor, likely exhibits moderate bioavailability; detailed PK parameters (half-life, clearance) not reported in current literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data not reported; as a Drp1 inhibitor, potential off-target effects include alterations in mitochondrial dynamics in non-target tissues; standard safety pharmacology studies would be required.
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| References | |
| Additional Infomation |
DRP1i27 is a research tool for mitochondrial biology; has not entered clinical trials or received marketing approval; not a therapeutic agent. For research use only.
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| Molecular Formula |
C20H28CL2N6O
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|---|---|
| Molecular Weight |
439.38
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| Related CAS # |
DRP1i27;1453028-33-5
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| Appearance |
Light yellow to brown solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.2759 mL | 11.3797 mL | 22.7593 mL | |
| 5 mM | 0.4552 mL | 2.2759 mL | 4.5519 mL | |
| 10 mM | 0.2276 mL | 1.1380 mL | 2.2759 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
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