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

Lintitript  (Synonyms: SR 27897)

Cat. No.: HY-101764 Purity: ≥99.0%
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Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin.

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

Lintitript Chemical Structure

Lintitript Chemical Structure

CAS No. : 136381-85-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 550 In-stock
Solution
10 mM * 1 mL in DMSO USD 550 In-stock
Solid
1 mg USD 238 In-stock
5 mg USD 500 In-stock
10 mg USD 850 In-stock
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Based on 1 publication(s) in Google Scholar

Lintitript Related Antibodies

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Description

Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin[1][2][3].

IC50 & Target

EC50: 6 nM (cholecystokinin (CCK1) receptor)[2]; Ki: 0.2 nM (cholecystokinin (CCK1) receptor)[1]
In Vitro

In vitro, Lintitript (SR 27897) is a competitive antagonist of cholecystokinin (CCK)-stimulated amylase release in isolated rat pancreatic acini (pA2 = 7.50) and of CCK-induced guinea pig gall bladder contractions (pA2 = 9.57)[1].
Lintitript produces concentration dependent inhibition of [125I]CCK binding to CCK1 receptor sites in the rat pancreas (IC50 value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC2 value of 479 nM). Lintitript inhibits [125I]gastrin binding to gastrin receptors. Lintitript (0.5 nM) increases the dissociation constant of CCK for the CCK A receptor (Kd = 1.8 to 7.2 nM) without modifying the maximum number of receptors (Bmax = 1800 to 1770 fmol/mg)[1].

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

Lintitript Related Antibodies
In Vivo

Lintitript (SR 27897; 1 mg/kg, i.v.) completely reverses the CCK-induced amylase secretion. Lintitript also inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 μg/kg, respectively). Lintitript is also very active (ED50 = 27 μg/kg p.o.) in the gall bladder emptying protocol with egg yolk as an inducer of endogenous CCK release[1].

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

411.86

Formula

C20H14ClN3O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CN1C(C(NC2=NC(C3=CC=CC=C3Cl)=CS2)=O)=CC4=C1C=CC=C4
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 (242.80 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 2.4280 mL 12.1400 mL 24.2801 mL
5 mM 0.4856 mL 2.4280 mL 4.8560 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.

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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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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

Purity: 99.58%

SDS (251 KB)

COA (252 KB) LCMS (120 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 2.4280 mL 12.1400 mL 24.2801 mL 60.7002 mL
5 mM 0.4856 mL 2.4280 mL 4.8560 mL 12.1400 mL
10 mM 0.2428 mL 1.2140 mL 2.4280 mL 6.0700 mL
15 mM 0.1619 mL 0.8093 mL 1.6187 mL 4.0467 mL
20 mM 0.1214 mL 0.6070 mL 1.2140 mL 3.0350 mL
25 mM 0.0971 mL 0.4856 mL 0.9712 mL 2.4280 mL
30 mM 0.0809 mL 0.4047 mL 0.8093 mL 2.0233 mL
40 mM 0.0607 mL 0.3035 mL 0.6070 mL 1.5175 mL
50 mM 0.0486 mL 0.2428 mL 0.4856 mL 1.2140 mL
60 mM 0.0405 mL 0.2023 mL 0.4047 mL 1.0117 mL
80 mM 0.0304 mL 0.1518 mL 0.3035 mL 0.7588 mL
100 mM 0.0243 mL 0.1214 mL 0.2428 mL 0.6070 mL
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Lintitript 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:

Lintitript136381-85-6SR 27897SR27897SR-27897Cholecystokinin ReceptorCCK ReceptorLong durationamylasegastricgallbladderemptyingleptinfoodintakeinsulingastrinInhibitorinhibitorinhibit

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