2. GPCR/G Protein Neuronal Signaling
  3. Cholecystokinin Receptor
  4. Devazepide

Devazepide  (Synonyms: L-364,718; MK-329)

Cat. No.: HY-106301 Purity: 99.58%
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Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders.

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

Devazepide Chemical Structure

Devazepide Chemical Structure

CAS No. : 103420-77-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 165 In-stock
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25 mg USD 450 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Devazepide:

Devazepide Related Antibodies

Top Publications Citing Use of Products

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CCKAR CCKBR

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders[1].

IC50 & Target

IC50: 45 pM (Rat pancreatic CCK receptor), 81 pM (Bovine gallbladder CCK receptor), 245 nM (Guinea pig brain CCK receptor)[1]
In Vivo

Devazepide (oral gavage; 4 mg/kg; twice per day) significantly accelerates cholesterol crystallization and crystal growth to microlithiasis, and the formation of gallstones in mice[2].
Devazepide (intraperitoneal injection; 0.1-1 mg/kg) has opposite effects on spontaneous locomotor activity, and on caerulein- and apomorphine-induced hypomotility in the mouse[3].

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

Animal Model: Male C57BL/6J mice[2]
Dosage: 4 mg/kg
Administration: Oral gavage; 4 mg/kg; twice per day
Result: Increased susceptibility to gallstone formation by impairing gallbladder emptying function.
Disrupted biliary cholesterol metabolism and enhanced intestinal cholesterol absorption in mice.
Molecular Weight

408.45

Formula

C25H20N4O2
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=CC2=C(C=CC=C2)N1)N[C@H]3N=C(C4=CC=CC=C4)C5=CC=CC=C5N(C)C3=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (489.66 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 2.4483 mL 12.2414 mL 24.4828 mL
5 mM 0.4897 mL 2.4483 mL 4.8966 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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% (20% SBE-β-CD in Saline)

    Solubility: 5 mg/mL (12.24 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

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

    Solubility: ≥ 5 mg/mL (12.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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
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 (sealed storage, away from moisture and light). 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 2.4483 mL 12.2414 mL 24.4828 mL 61.2070 mL
5 mM 0.4897 mL 2.4483 mL 4.8966 mL 12.2414 mL
10 mM 0.2448 mL 1.2241 mL 2.4483 mL 6.1207 mL
15 mM 0.1632 mL 0.8161 mL 1.6322 mL 4.0805 mL
20 mM 0.1224 mL 0.6121 mL 1.2241 mL 3.0604 mL
25 mM 0.0979 mL 0.4897 mL 0.9793 mL 2.4483 mL
30 mM 0.0816 mL 0.4080 mL 0.8161 mL 2.0402 mL
40 mM 0.0612 mL 0.3060 mL 0.6121 mL 1.5302 mL
50 mM 0.0490 mL 0.2448 mL 0.4897 mL 1.2241 mL
60 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0201 mL
80 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7651 mL
100 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6121 mL
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Devazepide 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:

Devazepide103420-77-5L-364,718 MK-329MK329MK 329MK-329Cholecystokinin ReceptorCCK ReceptorInhibitorinhibitorinhibit

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