| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| ln Vitro |
When D-3263 hydrochloride binds to and activates TRPM8, it can cause an increase in the entry of calcium and sodium, disturb the balance between calcium and sodium, and cause tumor cells that express TRPM8 to die. The inhibitory effects of D-3263 hydrochloride on prostate cancer and BPH may be partially attributed to a possible reduction in dihydrotestosterone (DHT) levels [1].
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| References | |
| Additional Infomation |
Enteric-coated TRPM8 agonist D-3263 hydrochloride is an enteric-coated, orally bioavailable formulation of a small molecule agonist of transient receptor potential melastatin 8 (TRPM8 or Trp-p8) with potential antitumor activity. The active ingredient of enteric-coated TRPM8 agonist D-3263 hydrochloride binds to and activates TRPM8, leading to increased calcium and sodium influx, calcium and sodium homeostasis disturbances, and death in TRPM8-expressing tumor cells. This drug may lower 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 normally expressed in prostate cells and appears to be overexpressed in benign prostatic hyperplasia (BPH) and prostate cancer.
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| Molecular Formula |
C21H31N3O3
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|---|---|
| Molecular Weight |
373.4891
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| Exact Mass |
409.213
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| CAS # |
1008763-54-9
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| Related CAS # |
D-3263;947257-66-1
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| PubChem CID |
49787136
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
553
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C[C@@H]1CC[C@H]([C@@H](C1)C(=O)N2C3=C(C=C(C=C3)OC)N(C2=O)CCN)C(C)C.Cl
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| InChi Key |
DYMRNRVXSXCQHZ-UANXYBPYSA-N
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| InChi Code |
InChI=1S/C21H31N3O3.ClH/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;1H/t14-,16+,17-;/m1./s1
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| Chemical Name |
3-(2-aminoethyl)-5-methoxy-1-[(1R,2S,5R)-5-methyl-2-propan-2-ylcyclohexanecarbonyl]benzimidazol-2-one;hydrochloride
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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, avoid exposure to moisture. |
| 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) |
DMSO : ~140 mg/mL (~341.51 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 14 mg/mL (34.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 140.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 3.5 mg/mL (8.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 35.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3.5 mg/mL (8.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6774 mL | 13.3872 mL | 26.7745 mL | |
| 5 mM | 0.5355 mL | 2.6774 mL | 5.3549 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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