2. GPCR/G Protein Neuronal Signaling
  3. Cholecystokinin Receptor
  4. L-365260 hemihydrate

L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors.

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L-365260 hemihydrate Chemical Structure

L-365260 hemihydrate Chemical Structure

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Based on 1 publication(s) in Google Scholar

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L-365260 hemihydrate Related Antibodies

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1 Publications Citing Use of MCE L-365260 hemihydrate

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Description

L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors[1][2][3].

IC50 & Target

Ki: 1.9 nM (gastrin); 2.0 nM (CCK-B)[1].
In Vitro

L-365260 hemihydrate exhibits a similar high affinity for brain CCK-B receptors of rats, mice and man, and a lower affinity for gastrin and brain CCK-B (IC50=20-40 nM) receptors in dog tissues[1].
L-365260 (1 μM) hemihydrate strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron[2].

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

L-365260 hemihydrate Related Antibodies
In Vivo

L-365260 hemihydrate (0.1-30 mg/kg; p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED50=0.03 mg/kg), rats (ED50=0.9 mg/kg) and guinea pigs (ED50=5.1 mg/kg)[1].
L-365260 hemihydrate (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats[3].
L-365260 hemihydrate (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats[3].

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

Animal Model: Male Sprague-Dawley rats (300-350 g; Morphine- injected)[3].
Dosage: 0.01, 0.05, 0.1, 0.2, 0.75, 1.0, 10.0 mg/kg
Administration: S.c. 10 min prior to i.p. injection of 4 mg/kg Morphine
Result: Enhanced morphine analgesia.
Molecular Weight

407.47

Formula

C24H24N4O3
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=CC(C)=C1)N[C@H]2C(N(C)C3=CC=CC=C3C(C4=CC=CC=C4)=N2)=O.[1/2].O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (122.71 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 2.4542 mL 12.2708 mL 24.5417 mL
5 mM 0.4908 mL 2.4542 mL 4.9083 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). 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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). 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 2.4542 mL 12.2708 mL 24.5417 mL 61.3542 mL
5 mM 0.4908 mL 2.4542 mL 4.9083 mL 12.2708 mL
10 mM 0.2454 mL 1.2271 mL 2.4542 mL 6.1354 mL
15 mM 0.1636 mL 0.8181 mL 1.6361 mL 4.0903 mL
20 mM 0.1227 mL 0.6135 mL 1.2271 mL 3.0677 mL
25 mM 0.0982 mL 0.4908 mL 0.9817 mL 2.4542 mL
30 mM 0.0818 mL 0.4090 mL 0.8181 mL 2.0451 mL
40 mM 0.0614 mL 0.3068 mL 0.6135 mL 1.5339 mL
50 mM 0.0491 mL 0.2454 mL 0.4908 mL 1.2271 mL
60 mM 0.0409 mL 0.2045 mL 0.4090 mL 1.0226 mL
80 mM 0.0307 mL 0.1534 mL 0.3068 mL 0.7669 mL
100 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6135 mL
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L-365260 hemihydrate 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:

L-365260 hemihydrateCholecystokinin ReceptorCCK ReceptorgastrinbraincholecystokininCCK-BanalgesiaInhibitorinhibitorinhibit

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