| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
EC50: 10.5 μM (TPC2)[2]
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|---|---|
| ln Vitro |
Ancient members of the voltage-gated ion channel superfamily are known as two-pore channels (TPC1-3). TPCs govern the trafficking of many payloads and are expressed throughout the endo-lysosomal system[1]. Depending on how it is triggered, TPC2 can mediate various physiological and potentially pathological effects. TPC2's ion selectivity is agonist-dependent rather than fixed. One special type of ion channel that responds to various activating ligands by conducting distinct ions is TPC2[1]. Does TPC2-A1- P (10 μM) consistently elicit Ca2+?signals, and compared to TPC2-A1-N, the TPC2-A1-P response reaches its plateau more slowly. The 50th EC?In a cell line that consistently expresses TPC2L11A/L12A, the entire concentration-effect relationships for the plateau response are 10.5 μM for TPC2-A1-P. TPC2-A1-P generates Ca2+ at 10-30 μM?signals in Hela cells that express TPC2 when extracellular Ca2+ is present but not absent. In contrast to TPC2-A1-N, the reactions are smaller and more gradual, which is in line with the outcomes seen in cells that express TPC2L11A/L12A stable. Can't TPC2-A1-P induce Ca2+?signals in cells that do not elicit Ca2+ influx and express "pore-dead" TPC2L11A/L12A/L265P?signals were redirected to the plasma membrane (TRPML1ΔNC) in cells expressing human TRPML1[1]. Endo-lysosomes isolated from cells expressing TPC2 and TPC2M484L exhibit currents evoked by TPC2-A1-P (10 μM) in endo-lysosomal patch-clamp experiments. The currents evoked by TPC2-A1-P are significantly larger than those evoked by TPC2-A1-N in both wild-type and gain-of-function variant, and exhibit an EC50?0.6 μM was the result for TPC2-A1 -P[1].
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| References |
[1]. Susanne Gerndt, et al. Agonist-mediated switching of ion selectivity in TPC2 differentially promotes lysosomal function. Elife. 2020 Mar 16;9:e54712.
[2]. Gerndt S, et al. Discovery of lipophilic two-pore channel agonists. FEBS J. 2020;287(24):5284-5293. [3]. Xuhui Jin, et al. Targeting Two-Pore Channels: Current Progress and Future Challenges. Trends Pharmacol Sci. 2020 Aug;41(8):582-594. |
| Molecular Formula |
C20H21BRF3NO3
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|---|---|
| Molecular Weight |
460.28
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| CAS # |
2804595-86-4
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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 |
| 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: 50 mg/mL (108.63 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.43 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1726 mL | 10.8630 mL | 21.7259 mL | |
| 5 mM | 0.4345 mL | 2.1726 mL | 4.3452 mL | |
| 10 mM | 0.2173 mL | 1.0863 mL | 2.1726 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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