2. GPCR/G Protein Neuronal Signaling
  3. Cholecystokinin Receptor
  4. CI-988 hemihydrate

CI-988 hemihydrate  (Synonyms: PD134308 hemihydrate)

Cat. No.: HY-105226B
Handling Instructions

Molarity Calculator

CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects.

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

CI-988 hemihydrate Chemical Structure

CI-988 hemihydrate Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of CI-988 hemihydrate:

CI-988 hemihydrate Related Antibodies

Top Publications Citing Use of Products

View All Cholecystokinin Receptor Isoform Specific Products:

View All Isoforms
CCKAR CCKBR

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects[1][2][3].

In Vitro

CI-988 inhibits specific 125I-BH-CCK-8 binding to NCI-H727 cells with high affinity (Ki of 4.5 nM). The increase in ROS caused by CCK-8 addition to NCI-727 cells is blocked significantly by CI-988. CI-988 (3 µM) inhibits the basal growth of NCI-H727 cells or that stimulated by CCK-8. CI-988 inhibits the ability of CCK-8 to cause ERK phosphorylation and elevate cytosolic Ca2+[1].
CI-988 inhibits in a dose-dependent manner the ability of CCK-8 to cause EGFR transactivation in NCI-H727 cells. CI-988 at doses of 1 and 10 µM weakly and strongly, respectively, inhibits the ability of 0.1µM CCK-8 to increase EGFR tyrosine phosphorylation. CI-988 antagonizes the ability of CCK-8 to cause lung cancer EGFR or ERK tyrosine phosphorylation[1].

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

CI-988 hemihydrate Related Antibodies
In Vivo

CI-988 (10 mg/kg; p.o.; daily; for 20 days) inhibits the growth of colorectal cancer in xenografts model mice[3].

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

Animal Model: Nude mice injected with LoVo cells[3]
Dosage: 10 mg/kg
Administration: p.o.; daily; for 20 days
Result: Inhibited the growth of xenografts by 53%.
Molecular Weight

623.74

Formula

C35H42N4O6.1/2H2O
Appearance

Solid

SMILES

OC(CCC(N[C@H](C1=CC=CC=C1)CNC([C@](CC2=CNC3=C2C=CC=C3)(C)NC(OC4[C@H]5C[C@H](C6)C[C@@H]4C[C@H]6C5)=O)=O)=O)=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 : ≥ 62.374 mg/mL (100.00 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 1.6032 mL 8.0162 mL 16.0323 mL
5 mM 0.3206 mL 1.6032 mL 3.2065 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.

  • 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 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.
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 1.6032 mL 8.0162 mL 16.0323 mL 40.0808 mL
5 mM 0.3206 mL 1.6032 mL 3.2065 mL 8.0162 mL
10 mM 0.1603 mL 0.8016 mL 1.6032 mL 4.0081 mL
15 mM 0.1069 mL 0.5344 mL 1.0688 mL 2.6721 mL
20 mM 0.0802 mL 0.4008 mL 0.8016 mL 2.0040 mL
25 mM 0.0641 mL 0.3206 mL 0.6413 mL 1.6032 mL
30 mM 0.0534 mL 0.2672 mL 0.5344 mL 1.3360 mL
40 mM 0.0401 mL 0.2004 mL 0.4008 mL 1.0020 mL
50 mM 0.0321 mL 0.1603 mL 0.3206 mL 0.8016 mL
60 mM 0.0267 mL 0.1336 mL 0.2672 mL 0.6680 mL
80 mM 0.0200 mL 0.1002 mL 0.2004 mL 0.5010 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CI-988 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:

CI-988 hemihydratePD134308 hemihydrateCholecystokinin ReceptorCCK ReceptorCCK-8CCK2RERKEGFRphosphorylationCa2+anxiolyticanti-tumorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CI-988 hemihydrate
Cat. No.:
HY-105226B
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.