| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
D-3263 increases calcium flux and cell death in cells expressing TRPM8 in vitro [1].
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|---|---|
| ln Vivo |
D-3263 alone (50 or 100 mg/kg/d) or in combination with finasteride (10 mg/kg/d) decreases prostatic hyperplasia in rats with evidence of dosage response. The maximum dose of the TRPM8 agonist D-3263 combined with finasteride resulted in lower prostate weight than the highest dose of D-3263 or finasteride alone, suggesting a potential additive effect [1].
|
| References | |
| Additional Infomation |
TRPM8 Agonist D-3263 is a small-molecule agonist for transient receptor potential melastatin member 8 (TRPM8 or Trp-p8), with potential antineoplastic activity. Upon administration, TRPM8 agonist D-3263 targets, binds to and activates TRPM8, which may result in an increase in intracellular calcium and sodium influx; the disruption of calcium and sodium homeostasis; and the induction of cell death in TRPM8-expressing tumor cells. This agent may decrease dihydrotestosterone (DHT) levels, which may contribute to its inhibitory effects on prostate cancer and benign prostatic hyperplasia (BPH). TRPM8 is a transmembrane calcium channel protein that is normally expressed in prostate cells and appears to be overexpressed in BPH and in prostate cancer.
|
| Molecular Formula |
C21H31N3O3
|
|---|---|
| Molecular Weight |
373.497
|
| Exact Mass |
373.237
|
| CAS # |
947257-66-1
|
| Related CAS # |
D-3263 hydrochloride;1008763-54-9
|
| PubChem CID |
44137358
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
3.819
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
27
|
| Complexity |
553
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
O=C([C@]1([H])C([H])([H])[C@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[C@]1([H])C([H])(C([H])([H])[H])C([H])([H])[H])N1C(N(C([H])([H])C([H])([H])N([H])[H])C2C([H])=C(C([H])=C([H])C1=2)OC([H])([H])[H])=O
|
| InChi Key |
ZGTYTFYRCIRWBL-HYVNUMGLSA-N
|
| InChi Code |
InChI=1S/C21H31N3O3/c1-13(2)16-7-5-14(3)11-17(16)20(25)24-18-8-6-15(27-4)12-19(18)23(10-9-22)21(24)26/h6,8,12-14,16-17H,5,7,9-11,22H2,1-4H3/t14-,16+,17-/m1/s1
|
| Chemical Name |
3-(2-aminoethyl)-5-methoxy-1-[(1R,2S,5R)-5-methyl-2-propan-2-ylcyclohexanecarbonyl]benzimidazol-2-one
|
| Synonyms |
D-3263; D 3263; D3263
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.6774 mL | 13.3869 mL | 26.7738 mL | |
| 5 mM | 0.5355 mL | 2.6774 mL | 5.3548 mL | |
| 10 mM | 0.2677 mL | 1.3387 mL | 2.6774 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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