2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. YM022

YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.

For research use only. We do not sell to patients.

YM022 Chemical Structure

YM022 Chemical Structure

CAS No. : 145084-28-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 398 In-stock
Solution
10 mM * 1 mL in DMSO USD 398 In-stock
Solid
5 mg USD 350 In-stock
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Based on 2 publication(s) in Google Scholar

YM022 Related Antibodies

Top Publications Citing Use of Products

View All CCR Isoform Specific Products:

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Purity & Documentation

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Description

YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively[1]. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo[3].

IC50 & Target[1]

CCR2

68 pM (Ki)

CCR1

63 nM (Ki)

In Vitro

YM022 inhibits binding to canine pancreas CCK-A receptor in a dose-dependent manner, with an IC50 value for [3H]devazepide binding of 136 nM[1].
YM022 inhibits the binding of [125I]CCK-8 to canine cloned gastrin/CCK-B receptor in a dose-dependent manner, with an IC50 value for [125I]CCK-8 binding of 0.73 nM[1].
Selectivity [ratio of (IC50 for gastrin/CCK-B receptor)/(IC50for CCK-A receptor)] of YM022 is 186[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

YM022 Related Antibodies
In Vivo

YM022 (intravenous injection; 0.01-1 μM/kg) dose-dependently inhibits pentagastrin- and peptone meal-induced acid secretion with ED50 values of 0.0261 and 0.0654 μmol/kg, respectively, without affecting histamine- or methacholine-induced acid secretion[3].
YM022 (subcutaneous injection; 300 μmol/kg; single dose) lowers the oxyntic mucosal HDC activity and raises the serum gastrin concentration in a dose-dependent manner (measured 24 h after dosage). Maximum enzyme inhibition is achieved at a dose of 300 μmol/kg  for YM022 and the inhibition of HDC lasts for 4 weeks. At sacrifice, drug residues can be seen at the injection site for as long as 4 (YM022) weeks after injection in rat[3].
YM022 is suspended in 2% Methocel for oral ingestion and in PEG300 for subcutaneous injection[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat[3]
Dosage: 300 μmol/kg
Administration: Subcutaneous injection; 300 μmol/kg; single dose
Result: Suppressed the ECL cell activity for at least 4 as manifested in greatly reduced HDC activity, greatly elevated serum gastrin level.
Molecular Weight

516.59

Formula

C32H28N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=CC(C)=C1)N[C@H]2C(N(CC(C3=CC=CC=C3C)=O)C4=CC=CC=C4C(C5=CC=CC=C5)=N2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (193.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9358 mL 9.6789 mL 19.3577 mL
5 mM 0.3872 mL 1.9358 mL 3.8715 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.93%

SDS (420 KB)

COA (261 KB) HNMR (120 KB) RP-HPLC (269 KB) LCMS (414 KB) Elemental Analysis Report (119 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9358 mL 9.6789 mL 19.3577 mL 48.3943 mL
5 mM 0.3872 mL 1.9358 mL 3.8715 mL 9.6789 mL
10 mM 0.1936 mL 0.9679 mL 1.9358 mL 4.8394 mL
15 mM 0.1291 mL 0.6453 mL 1.2905 mL 3.2263 mL
20 mM 0.0968 mL 0.4839 mL 0.9679 mL 2.4197 mL
25 mM 0.0774 mL 0.3872 mL 0.7743 mL 1.9358 mL
30 mM 0.0645 mL 0.3226 mL 0.6453 mL 1.6131 mL
40 mM 0.0484 mL 0.2420 mL 0.4839 mL 1.2099 mL
50 mM 0.0387 mL 0.1936 mL 0.3872 mL 0.9679 mL
60 mM 0.0323 mL 0.1613 mL 0.3226 mL 0.8066 mL
80 mM 0.0242 mL 0.1210 mL 0.2420 mL 0.6049 mL
100 mM 0.0194 mL 0.0968 mL 0.1936 mL 0.4839 mL
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YM022 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM022145084-28-2YM 022YM-022CCRCC chemokine receptorgastric acidsecretionhistidine decarboxylaseInhibitorinhibitorinhibit

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