| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
ZINC-3573 targets the Mas-related G protein-coupled receptor X2 (MRGPRX2), a receptor involved in pain and itch signaling. It is a selective agonist of MRGPRX2 with an EC50 of 740 nM. By activating MRGPRX2, ZINC-3573 induces mast cell degranulation and calcium release.
|
|---|---|
| ln Vitro |
In LAD2 mast cells, (R)-ZINC-3573 (0.001 nM-100 μM) stimulates intracellular calcium release and β-hexosaminidase degranulation [1].
ZINC-3573 is a selective MRGPRX2 agonist with an EC50 of 740 nM. It activates endogenous MRGPRX2 in human mast cell lines, inducing cell degranulation and calcium release. At concentrations of 0.001 nM to 100 µM, (R)-ZINC-3573 promotes β-hexosaminidase degranulation and induces intracellular calcium release in LAD2 mast cells. |
| ln Vivo |
Specific in vivo activity data for ZINC-3573 are not extensively reported in the available literature. As a MRGPRX2 agonist, it may be useful for studying pain and itch in animal models. Further research is needed to characterize its pharmacokinetic and pharmacodynamic profiles in animal models.
|
| Enzyme Assay |
The in vitro receptor binding or functional assay for ZINC-3573 typically involves measuring its activity at MRGPRX2 using standard cell-based assays. Cells expressing MRGPRX2 are treated with varying concentrations of the compound, and receptor activation is measured by assessing calcium release or other downstream signaling pathways. The EC50 value is determined from the dose-response curve.
|
| Cell Assay |
The in vitro cellular assay for ZINC-3573 typically involves culturing human mast cell lines such as LAD2 in appropriate growth media. Cells are treated with varying concentrations of the compound, and mast cell degranulation is assessed by measuring β-hexosaminidase release. Intracellular calcium release is measured using fluorescent calcium indicators.
|
| Animal Protocol |
In vivo animal studies for ZINC-3573 would typically involve the use of rodent models of pain or itch. Animals would be administered the compound via appropriate routes (e.g., intradermal or subcutaneous injection) at various dose levels. Pain responses would be assessed using standard pain tests, and itch responses would be assessed by measuring scratching behavior.
|
| ADME/Pharmacokinetics |
ZINC-3573 has a molecular weight of 307.4 g/mol and a molecular formula of C18H21N5. The compound is also known as (R)-ZINC-3573 and ZINC 3573. Further detailed physicochemical properties are available from the manufacturer's data sheets. The compound is intended for research use only.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for ZINC-3573 are not available in the public domain. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. Standard safety assessments would be required before any clinical application. Researchers should consult the safety data sheet for detailed handling and disposal information.
|
| References | |
| Additional Infomation |
ZINC-3573 is a selective Mas-related G protein-coupled receptor X2 (MRGPRX2) agonist with an EC50 of 740 nM. It can be used as a MRGPRX2 probe for the research of pain and itch. (R)-ZINC-3573 activates endogenous MRGPRX2 in human mast cell lines, inducing cell degranulation and calcium release. It has not yet entered clinical trials and is strictly for preclinical research purposes.
|
| Molecular Formula |
C18H21N5
|
|---|---|
| Molecular Weight |
307.392843008041
|
| Exact Mass |
307.179
|
| Elemental Analysis |
C, 70.33; H, 6.89; N, 22.78
|
| CAS # |
2089389-15-9
|
| Related CAS # |
2089389-15-9 (R-isomer);1378183-16-4 (racemic mixture);
|
| PubChem CID |
95882507
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Index of Refraction |
1.671
|
| LogP |
1.36
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
23
|
| Complexity |
395
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
N1(C2=CC(C3C=CC=CC=3)=NC3=CC=NN23)CC[C@H](C1)N(C)C
|
| InChi Key |
XKBSPAZCFAIBJL-OAHLLOKOSA-N
|
| InChi Code |
InChI=1S/C18H21N5/c1-21(2)15-9-11-22(13-15)18-12-16(14-6-4-3-5-7-14)20-17-8-10-19-23(17)18/h3-8,10,12,15H,9,11,13H2,1-2H3/t15-/m1/s1
|
| Chemical Name |
(3R)-N,N-dimethyl-1-(5-phenylpyrazolo[1,5-a]pyrimidin-7-yl)pyrrolidin-3-amine
|
| Synonyms |
ZINC-3573; ZINC 3573; ZINC3573.
|
| 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) |
DMSO : ~50 mg/mL (~162.66 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.13 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 | 3.2532 mL | 16.2660 mL | 32.5320 mL | |
| 5 mM | 0.6506 mL | 3.2532 mL | 6.5064 mL | |
| 10 mM | 0.3253 mL | 1.6266 mL | 3.2532 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
