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

Sograzepide  (Synonyms: Netazepide; YF 476; YM-220)

Cat. No.: HY-14850 Purity: 98.35%
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Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.

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Sograzepide Chemical Structure

Sograzepide Chemical Structure

CAS No. : 155488-25-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 275 In-stock
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10 mg USD 450 In-stock
50 mg USD 1400 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Sograzepide:

Sograzepide Related Antibodies

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Description

Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM[1]. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively[2].

IC50 & Target

IC50: 0.1 nM (Gastrin/CCK-B); 501 nM (Gastrin/CCK-A)[1]
In Vivo

Sograzepide (Netazepide; YF 476; YM-220) (0.1 μmol/kg; intravenous injection) has an inhibition effect on pentagastrin-induced gastric acid secretion in anethsetized rats with an ED50 of 87 nmol/kg[1].
Sograzepide (Netazepide; YF 476; YM-220) (intravenous injection; 10 μM/kg) inhibits pentagastrin-induced acid secretion with an ED50 value of 0.0086 μM/kg, but does not affect histamine- and bethanechol-induced acid secretion[2].
Sograzepide (Netazepide; YF 476; YM-220) (intravenous injection; oral administration) in Heidenhain pouch dogs, inhibits pentagastrin-stimulated gastric acid secretion in a dose-dependent manner with ED50 values of 0.018 and 0.020 μM/kg, respectively [2].

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

498.58

Formula

C28H30N6O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=CC=CC(NC)=C1)N[C@H]2C(N(CC(C(C)(C)C)=O)C3=CC=CC=C3C(C4=NC=CC=C4)=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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (200.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0057 mL 10.0285 mL 20.0570 mL
5 mM 0.4011 mL 2.0057 mL 4.0114 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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: 98.35%

COA (258 KB) LCMS (268 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0057 mL 10.0285 mL 20.0570 mL 50.1424 mL
5 mM 0.4011 mL 2.0057 mL 4.0114 mL 10.0285 mL
10 mM 0.2006 mL 1.0028 mL 2.0057 mL 5.0142 mL
15 mM 0.1337 mL 0.6686 mL 1.3371 mL 3.3428 mL
20 mM 0.1003 mL 0.5014 mL 1.0028 mL 2.5071 mL
25 mM 0.0802 mL 0.4011 mL 0.8023 mL 2.0057 mL
30 mM 0.0669 mL 0.3343 mL 0.6686 mL 1.6714 mL
40 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2536 mL
50 mM 0.0401 mL 0.2006 mL 0.4011 mL 1.0028 mL
60 mM 0.0334 mL 0.1671 mL 0.3343 mL 0.8357 mL
80 mM 0.0251 mL 0.1254 mL 0.2507 mL 0.6268 mL
100 mM 0.0201 mL 0.1003 mL 0.2006 mL 0.5014 mL
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Sograzepide 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:

Sograzepide155488-25-8Netazepide YF 476 YM-220YF476YF 476YF-476YM220YM 220YM-220Cholecystokinin ReceptorCCK ReceptorgastricacidsecretionInhibitorinhibitorinhibit

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