| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized Powder |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 3-(2-aminoethyl)-5-methoxy-1-[(1R,2S,5R)-5-methyl-2-propan-2-ylcyclohexanecarbonyl]benzimidazol-2-one; hydrochloride.
- CAS number: 1008763-54-9
- Molecular formula: C21H32ClN3O3.
- Purity: >97%
- Concentration: 1 nM - 10 µM.
- Form: Lyophilized Powder
- Solubility: Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
- Reconstitution: Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: TRPM8 channels
- Source: Synthetic
- Activity: D-3263 hydrochloride is a potent TRPM8 channel agonist1.It shows evidence of activity in preclinical tumor models and was tested in phase 1 clinical trials for the treatment of prostate cancer1-3.
Scientific background
D-3263 hydrochloride, is a potent agonist of the transient receptor potential melastatin-8 (TRPM8) channel1. Activation of the channel increases Ca2+ and Na+ entry and induces cell death in TRPM8-expressing tumor cells. This agent may decrease androstanolone (DHT) levels, which may contribute to its inhibitory effects on prostate cancer and prostatic hyperplasia1.The compound shows activity in preclinical tumor models and was tested in phase 1 clinical trials for the treatment of prostate cancer1.TRPM8 is a Ca2+-permeable channel, a member of the 'long' or melastatin (M) group of TRP proteins and is activated by temperatures by the range of 8-28°C or by cooling compounds. The TRPM8 gene is and up-regulated in prostate cancer and other malignancies. It is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons2,3.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
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