2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. CGP 12177

CGP 12177 ((±)-CGP 12177) is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 is a β3-AR (Ki = 88 nM) agonist with β1/β2-AR (Ki = 0.9 nM for β1; Ki = 4 nM for β2) antagonist action. CGP 12177 exhibits partial agonist properties for α1-AR in rat pulmonary artery. CGP 12177 regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 can be used for cardiovascular and metabolic disease research[1][2][3][4].

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

CGP 12177

CGP 12177 Chemical Structure

CAS No. : 81047-99-6

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

Other In-stock Forms of CGP 12177:

Other Forms of CGP 12177:

CGP 12177 Related Antibodies

Top Publications Citing Use of Products

View All Adrenergic Receptor Isoform Specific Products:

View All Isoforms
α adrenergic receptor β adrenergic receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CGP 12177 ((±)-CGP 12177) is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 is a β3-AR (Ki = 88 nM) agonist with β1/β2-AR (Ki = 0.9 nM for β1; Ki = 4 nM for β2) antagonist action. CGP 12177 exhibits partial agonist properties for α1-AR in rat pulmonary artery. CGP 12177 regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 can be used for cardiovascular and metabolic disease research[1][2][3][4].

IC50 & Target[1][4]

Beta-1 adrenergic receptor

0.9 nM (Ki)

Beta-2 adrenergic receptor

4 nM (Ki)

Beta-3 adrenergic receptor

88 nM (Ki)

α1-adrenergic receptor

 

In Vitro

CGP 12177 (0.01-100 μM) enhances tension induced by 3 μM Prostaglandin F2α (PGF2α) (HY-12956) in rat intralobar pulmonary arteries in a concentration-dependent manner, while inducing concentration-dependent relaxation when arteries precontracted with 30 nM Phenylephrine (PHE) (HY-B0769)[1].
CGP 12177 (0.01-100 μM) exerts only minor effect on rat intralobar pulmonary arteries under basal tone, but elicits contractile effects and markedly potentiates PHE-induced contraction in the presence of PGF2α (3 μM)[1].
CGP 12177 (1-100 μM) induces an increase in intracellular calcium concentration in rat pressurized arteries loaded with Fura pentakisester-3 (PE-3) and precontracted with PGF2α[1].
CGP 12177 (100 μM, 15 min) exhibits no significant effect on the basal tone in rat intralobar pulmonary arteries, but shifts the concentration-response curve to PHE to the right without any changes in the maximal response[1].
CGP 12177 (1–100 μM)-induced contractions in PGF2α-precontracted arteries are suppressed by Phentolamine (1 μM), Phenoxybenzamine (1 μM), SR 59230A (3 μM), and Bupranolol (5 μM) in rat intralobar pulmonary arteries[1].
CGP 12177 fully and concentration-dependently displaces [3H]prazosin-specific binding, with a pKi value of 5.22[1].
CGP 12177 (0-10 μM, 30 min) does not stimulate the internalization of GFP-tagged human β2-adrenoceptors in CHO-K1 cells[2].
CGP 12177 acts as a high-affinity partial agonist for cyclic AMP accumulation and cAMP response element (CRE)-mediated gene transcription in CHO-K1 cells expressing the human β2-adrenoceptor[2].

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

CGP 12177 Related Antibodies
In Vivo

CGP 12177 (0.05, 0.2, 0.5 and 1mg/kg, s.c., daily for 15 days) stimulates the expression of certain ucp genes and the leptin gene concomitantly in NMRI mice adipose tissues[3].

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

Animal Model: Male NMRI mice (4-weeks old)[3]
Dosage: 0.05, 0.2, 0.5 and 1mg/kg
Administration: s.c., daily for 15 days
Result: Significantly decreased expression of the mRNAs for UCP1, UCP2 and UCP3 in brown adipose tissue (BAT) at the lower doses compared to control.
Slightly increased expression of the mRNAs for UCP1, UCP2 and UCP3 in brown adipose tissue (BAT) at the higher doses compared to control.
Markedly enhanced UCP1 mRNA expression in both white adipose tissue (WAT) depots (inguinal IWAT and epididymal EWAT) in a dose-dependent manner, the increase was from low (and variable) basal levels in IWAT and from undetectable levels in EWAT of control animals.
Upregulated UCP3 mRNA expression in WAT especially in EWAT and, to a lesser extent, in IWAT.
Did not upregulated UCP2 mRNA expression in any WAT depot.
Showed a decreased expression of UCP2 mRNA at doses lower than 1mg/kg in both IWAT and EWAT.
Regulated leptin mRNA levels in a tissue-dependent manner.
Showed no effect on leptin mRNA levels in EWAT at any dose.
Showed a 3-fold increase of leptin mRNA levels in BAT at 0.5 and 1mg/kg.
Resulted in a maximum of 2-fold stimulation in IWAT at 0.5 mg/kg.
Did not have any apparent effect on food intake, body weight or the weight of the analysed fat depots at any dose tested.
Molecular Weight

279.33

Formula

C14H21N3O3
CAS No.
SMILES

O=C1NC2=C(OCC(O)CNC(C)(C)C)C=CC=C2N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • 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.

CGP 12177 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

CGP 1217781047-99-6(±)-CGP 12177CGP12177CGP-12177Adrenergic ReceptorBeta Receptorβ-ARβ2-ARβ1-ARsβ3-ARPGF2αα1-ARrat pulmonary arteryNMRI miceadipose tissuesInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CGP 12177
Cat. No.:
HY-101393
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

SAFETY DATA SHEET (SDS)

Request for HNMR Report

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