| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
CGS 21680 HCl (CGS21680; CGS-21680), the hydrochloride salt of CGS 21680, is a potent and specific agonist of adenosine A2 receptors with potential antideppressant activity. It has 140-fold selectivity over A1 receptors and an IC50 of 22 nM for adenosine A2 receptor activation.
| Targets |
Adenosine A2A receptor ( Ki = 27 nM )
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Cell Assay |
Each group's 10×106 MNCs are re-suspended in 2 mL of RPMI 1640. Carboxy-fluorescein diacetate, succinimidyl ester (CFSE, final concentration 2.5 μM) is added to cell suspensions and well mixed. The staining process is quenched by adding 10 mL of ice-cold complete RPMI 1640 (containing 10% FBS) and incubating on ice for 5 minutes after being incubated in the dark for 15 minutes at 37°C. The cells are then given two RPMI 1640 washes. Re-suspended cell pellets are in full RPMI 1640, which contains 10% FBS. In 24-well culture plates, the stained MNCs (1×106 cells/mL, 1 mL/well) are cultured in triplicate under 37°C dark conditions. 50 μL of either P0 peptide (final concentration 10 μg/mL) or Concanavalin A (ConA, final concentration 5 μg/mL) are added to each well. After 72 hours, cells are gathered and stained for 30 minutes at 4°C using an anti-rat CD4 antibody labeled with PE. Ultimately, a flow cytometer is used to examine the cells.
|
|
| Animal Protocol |
In the nearby animal facility, female Lewis rats, weighing between 140 and 160 grams at birth, are kept in housing designed to prevent pathogens and provide them with unrestricted access to food and water. Day 5 p.i. is when CGS21680 administration begins (at a dose of 1 mg/kg in PBS). Until the end of the trials, rats in the experimental group receive intraperitoneal (i.p.) injections of CGS21680 every two days. The control group of rats receives the same volume of PBS in the same manner. It is decided on the dosages (1 mg/kg/i.p.) and the treatment plan (every two days, beginning on day 5 p.i.).
|
|
| References |
| Molecular Formula |
C23H29N7O6.HCL
|
|
|---|---|---|
| Molecular Weight |
535.98
|
|
| Exact Mass |
535.19
|
|
| Elemental Analysis |
C, 51.54; H, 5.64; Cl, 6.61; N, 18.29; O, 17.91
|
|
| CAS # |
124431-80-7
|
|
| Related CAS # |
CGS 21680; 120225-54-9
|
|
| Appearance |
Solid powder
|
|
| SMILES |
CCNC(=O)[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=C(N=C32)NCCC4=CC=C(C=C4)CCC(=O)O)N)O)O.Cl
|
|
| InChi Key |
QPHVMNOEKKJYJO-MJWSIIAUSA-N
|
|
| InChi Code |
InChI=1S/C23H29N7O6.ClH/c1-2-25-21(35)18-16(33)17(34)22(36-18)30-11-27-15-19(24)28-23(29-20(15)30)26-10-9-13-5-3-12(4-6-13)7-8-14(31)32;/h3-6,11,16-18,22,33-34H,2,7-10H2,1H3,(H,25,35)(H,31,32)(H3,24,26,28,29);1H/t16-,17+,18-,22+;/m0./s1
|
|
| Chemical Name |
3-[4-[2-[[6-amino-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]purin-2-yl]amino]ethyl]phenyl]propanoic acid;hydrochloride
|
|
| Synonyms |
|
|
| 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) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% Propylene glycol , 5% Tween 80 , 65% D5W: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8657 mL | 9.3287 mL | 18.6574 mL | |
| 5 mM | 0.3731 mL | 1.8657 mL | 3.7315 mL | |
| 10 mM | 0.1866 mL | 0.9329 mL | 1.8657 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
COA