| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
CID-85469571 targets GPR18, acting as a potent and selective antagonist. By blocking GPR18, it inhibits signaling through this receptor. It exhibits >36-fold selectivity versus CB1 and GPR55 and 14-fold selectivity versus CB2 receptors. Its mechanism involves the competitive inhibition of GPR18 activation by endogenous ligands.
|
|---|---|
| ln Vitro |
In vitro, CID-85469571 antagonizes GPR18 with an IC50 of 0.279 μM. It exhibits >36-fold selectivity versus CB1 and GPR55 and 14-fold selectivity versus CB2 receptors. It has anti-inflammatory activity. Its activity is assessed in cell-based assays of GPR18 function.
|
| ln Vivo |
In vivo, CID-85469571 is used to study metabolic diseases and obesity. As a GPR18 antagonist, it has potential therapeutic applications in these areas. However, detailed in vivo efficacy data are limited. It is primarily used as a research tool.
|
| Enzyme Assay |
In vitro assays for CID-85469571 typically measure its binding to and antagonism of GPR18. Cell lines expressing recombinant GPR18 are treated with the compound, and receptor activation is assessed by measuring downstream signaling pathways, such as GTPγS binding or calcium mobilization. IC50 values are determined from dose-response curves.
|
| Cell Assay |
Cellular assays for CID-85469571 are performed using cells expressing GPR18. Cells are treated with the compound, and its effects on GPR18-mediated signaling are assessed. Its anti-inflammatory activity can be studied in immune cells by measuring cytokine production.
|
| Animal Protocol |
In vivo animal studies with CID-85469571 are conducted in models of obesity and metabolic disorders. The compound is administered to animals, and metabolic parameters such as body weight, glucose tolerance, and insulin sensitivity are measured. Its anti-inflammatory effects are also assessed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for CID-85469571 are limited. Its molecular weight is 384.88 g/mol and its formula is C20H17ClN2O2S. For research use, it is typically dissolved in DMSO for in vitro studies. Its oral bioavailability and metabolic stability have not been extensively characterized.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicological data for CID-85469571 are limited. In cell-based assays, the compound shows potent GPR18 antagonism. No significant toxicity has been reported at the doses used for receptor studies. The compound is intended for laboratory research only and should be handled with standard safety precautions.
|
| References | |
| Additional Infomation |
CID-85469571 (PSB-CB5) is a research compound used as a potent and selective GPR18 antagonist. It has anti-inflammatory activity and is used to study obesity and metabolic disorders. The compound is a valuable tool for investigating the role of GPR18 in various physiological and pathological processes. It is not approved for clinical use and is intended for laboratory research only.
|
| Molecular Formula |
C20H17CLN2O2S
|
|---|---|
| Molecular Weight |
384.88
|
| Exact Mass |
384.069
|
| CAS # |
1627710-30-8
|
| PubChem CID |
85469571
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
549.9±60.0 °C at 760 mmHg
|
| Flash Point |
286.4±32.9 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.672
|
| LogP |
4.43
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
26
|
| Complexity |
586
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC(=CC=1)COC1=CC=CC(=C1)/C=C1/C(N2C(=N/1)SCCC2)=O
|
| InChi Key |
XJBQRMOGMULGPP-PDGQHHTCSA-N
|
| InChi Code |
InChI=1S/C20H17ClN2O2S/c21-16-7-5-14(6-8-16)13-25-17-4-1-3-15(11-17)12-18-19(24)23-9-2-10-26-20(23)22-18/h1,3-8,11-12H,2,9-10,13H2/b18-12-
|
| Chemical Name |
(2Z)-2-[[3-[(4-chlorophenyl)methoxy]phenyl]methylidene]-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazin-3-one
|
| Synonyms |
CID 85469571; CID85469571; CID-85469571
|
| 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 | 2.5982 mL | 12.9911 mL | 25.9821 mL | |
| 5 mM | 0.5196 mL | 2.5982 mL | 5.1964 mL | |
| 10 mM | 0.2598 mL | 1.2991 mL | 2.5982 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
