| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
HEP-50768 (1 nM-1 μM; 30 min) effectively inhibited DCA-induced calcium mobilization in HEK293T cells stably expressing hX4, with an IC50 of 14 nM, and achieved 100% inhibition at 2 μM [1]. HEP-50768 (0.1 μM) as an inverse agonist significantly reduced the basal level of inositol monophosphate in HEK293T cells expressing hX4 [1]. HEP-50768 (2 μM; 1.5 h) slightly reduced the GTPase activity of the purified hX4-Gq complex, consistent with its inverse agonist activity [1]. HEP-50768 (0.02-50 nM) had high affinity for the purified apo hX4 and hX4-miniGαq complexes, with comparable affinity and K0 values of 0.6 nM and 0.7 nM, respectively [1]. HEP-50768 (0.1 nM-10 mM; 30 min) is highly selective for hX4, with weak inhibitory effects on hX1 (IC50 = 16 μM) and hX2 (IC50 = 1.5 μM), and has no agonist activity against either of these receptors [1]. HEP-50768 (~5 min) has minimal inhibitory effect on hERG channels in HEK293 cells that stably express hERG, with IC50 values exceeding 30 μM [1].
|
|---|---|
| ln Vivo |
HEP-50768 (5-10 mg/kg; orally; single dose; 2.5 hours before pruritus induction) significantly reduced DCA-3S-induced scratching behavior in hX4 humanized rats, demonstrating a strong antipruritic effect [1].
|
| Animal Protocol |
Animal/Disease Models:hX4 humanized rats (produced by hybridization of MRGA::hX4-Cre rats and Rosa26::lsl-hX4 rats) [1]
Doses: 5 mg/kg; 10 mg/kg Route of Administration: Oral; Single dose; 2.5 hours before pruritus induction Experimental Results: Compared with the PBS solvent control group, the number of scratches induced by DCA-3S was significantly reduced (P = 0.0059, 5 mg/kg dose). Compared with the PBS solvent control group, the number of scratches induced by DCA-3S was significantly reduced (P = 0.0049, 10 mg/kg dose). |
| References |
| Molecular Formula |
C16H10F4N4O
|
|---|---|
| Molecular Weight |
350.27
|
| CAS # |
3036387-75-1
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC1=C(C2=NN=NN2)C=CC=C1[C@@H]3CC4=CC(C(F)(F)F)=CC=C4O3
|
| 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 | 2.8549 mL | 14.2747 mL | 28.5494 mL | |
| 5 mM | 0.5710 mL | 2.8549 mL | 5.7099 mL | |
| 10 mM | 0.2855 mL | 1.4275 mL | 2.8549 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
