| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
|
YM-022 (YM022) is a novel and potent non-peptide CCK-BR (gastrin/cholecystokinin-B receptor) silent antagonist that can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo. It inhibits CCK-B and CCK-A receptors with Ki values of 68 pM and 63 nM, respectively.
| ln Vitro |
In a dose-dependent manner, YM022 blocks the binding of [3H]devazepide to the canine pancreatic CCK-A receptor; the IC50 value for this binding is 136 nM [1]. With an IC50 value of 0.73 nM for [125I]CCK-8 binding, YM022 inhibits [125I]CCK-8 binding to the canine cloned gastrin/CCK-B receptor in a dose-dependent manner [1]. YM022 has a selectivity of 186 [(IC50 of gastrin/CCK-B receptor)/(IC50 of CCK-A receptor)] [1].
|
|---|---|
| ln Vivo |
YM022 (i.v.; 0.01-1 μM/kg) dose-dependently reduces acid secretion caused by pentagastrin and peptone powder (ED50 values: 0.0261 and 0.0654 μmol/kg, respectively). acid secretion caused by a base, without affecting histamine or methachol. Base-induced acid secretion [3]. In a dose-dependent manner, YM022 (subcutaneous injection; 300 μmol/kg; single dose) raises blood gastrin concentrations (measured 24 hours after dosing) while decreasing oxyntic mucosal HDC activity. At 300 μmol/kg, YM022 exhibited the highest level of enzyme inhibition, and this suppression of HDC persisted for four weeks. Up to 4 (YM022) weeks of drug residue were seen at the injection site when the rats were slaughtered [3]. YM022 is suspended in PEG300 for subcutaneous injection and 2% Methocel for oral intake [3].
|
| Animal Protocol |
Animal/Disease Models: Rat[3]
Doses: 300 μmol/kg Route of Administration: subcutaneous injection; 300 μmol/kg; single dose Experimental Results: inhibits ECL cell activity for at least 4 hrs (hrs (hours)), manifested as a greatly diminished HDC activity, serum gastrin The level is greatly increased. |
| References |
|
| Molecular Formula |
C32H28N4O3
|
|---|---|
| Molecular Weight |
516.6
|
| Exact Mass |
516.216
|
| CAS # |
145084-28-2
|
| PubChem CID |
122130
|
| Appearance |
White to off-white solid powder
|
| Density |
1.23g/cm3
|
| Boiling Point |
735.4ºC at 760mmHg
|
| Melting Point |
187-190 °C
|
| Flash Point |
398.6ºC
|
| Vapour Pressure |
1.72E-21mmHg at 25°C
|
| Index of Refraction |
1.647
|
| LogP |
5.482
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
39
|
| Complexity |
913
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC1=CC(=CC=C1)NC(=O)N[C@H]2C(=O)N(C3=CC=CC=C3C(=N2)C4=CC=CC=C4)CC(=O)C5=CC=CC=C5C
|
| InChi Key |
YCXFHPUBGMMWJQ-PMERELPUSA-N
|
| InChi Code |
InChI=1S/C32H28N4O3/c1-21-11-10-15-24(19-21)33-32(39)35-30-31(38)36(20-28(37)25-16-7-6-12-22(25)2)27-18-9-8-17-26(27)29(34-30)23-13-4-3-5-14-23/h3-19,30H,20H2,1-2H3,(H2,33,35,39)/t30-/m0/s1
|
| Chemical Name |
1-(3-methylphenyl)-3-[(3R)-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]urea
|
| Synonyms |
YM022 YM 022 YM-022
|
| 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 : ~100 mg/mL (~193.58 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.84 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 | 1.9357 mL | 9.6787 mL | 19.3573 mL | |
| 5 mM | 0.3871 mL | 1.9357 mL | 3.8715 mL | |
| 10 mM | 0.1936 mL | 0.9679 mL | 1.9357 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
