CGP 12177 hydrochloride (Synonyms: (±)-CGP 12177 hydrochloride)

Cat. No.: HY-101393A Purity: 99.57%: Data Sheet
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CGP 12177 ((±)-CGP 12177) hydrochloride is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 hydrochloride is a β₃-AR (K_i = 88 nM) agonist with β₁/β₂-AR (K_i = 0.9 nM for β₁; K_i = 4 nM for β₂) antagonist action. CGP 12177 hydrochloride exhibits partial agonist properties for α₁-AR in rat pulmonary artery. CGP 12177 hydrochloride regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 hydrochloride 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 hydrochloride Chemical Structure

CAS No. : 64208-32-8

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Other Forms of CGP 12177 hydrochloride:

CGP 12177 Get quote

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α adrenergic receptor β adrenergic receptor

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Description

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) hydrochloride enhances tension induced by 3 μM Prostaglandin F_2α (PGF_2α) (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) hydrochloride 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 PGF_2α (3 μM)^[1].
CGP 12177 (1-100 μM) hydrochloride induces an increase in intracellular calcium concentration in rat pressurized arteries loaded with Fura pentakisester-3 (PE-3) and precontracted with PGF_2α^[1].
CGP 12177 (100 μM, 15 min) hydrochloride 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) hydrochloride-induced contractions in PGF_2α-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 hydrochloride fully and concentration-dependently displaces [³H]prazosin-specific binding, with a pK_i value of 5.22^[1].
CGP 12177 (0-10 μM, 30 min) hydrochloride does not stimulate the internalization of GFP-tagged human β₂-adrenoceptors in CHO-K1 cells^[2].
CGP 12177 hydrochloride 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.

In Vivo

CGP 12177 (0.05, 0.2, 0.5 and 1mg/kg, s.c., daily for 15 days) hydrochloride 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

315.80

Formula

C₁₄H₂₂ClN₃O₃

CAS No.

64208-32-8

Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=C(OCC(O)CNC(C)(C)C)C=CC=C2N1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°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 : 10 mg/mL (31.67 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	3.1666 mL	15.8328 mL	31.6656 mL
5 mM	0.6333 mL	3.1666 mL	6.3331 mL
10 mM	0.3167 mL	1.5833 mL	3.1666 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Purity & Documentation

Purity: 99.69%

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Data Sheet (281 KB) SDS (252 KB)

COA (252 KB) LCMS (87 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

[1]. Leblais V, et al. Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A, on the contraction of rat intrapulmonary artery. J Pharmacol Exp Ther. 2004 Apr;309(1):137-45. [Content Brief]

[2]. Baker JG, et al. Pharmacological characterization of CGP 12177 at the human beta(2)-adrenoceptor. Br J Pharmacol. 2002 Oct;137(3):400-8. [Content Brief]

[3]. Oliver P, et al. In vivo effects of CGP-12177 on the expression of leptin and uncoupling protein genes in mouse brown and white adipose tissues. Int J Obes Relat Metab Disord. 2000 Apr;24(4):423-8. [Content Brief]

[4]. Strosberg AD, et al. Function and regulation of the beta 3-adrenoceptor. Trends Pharmacol Sci. 1996 Oct;17(10):373-81. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1666 mL	15.8328 mL	31.6656 mL	79.1640 mL
	5 mM	0.6333 mL	3.1666 mL	6.3331 mL	15.8328 mL
	10 mM	0.3167 mL	1.5833 mL	3.1666 mL	7.9164 mL
	15 mM	0.2111 mL	1.0555 mL	2.1110 mL	5.2776 mL
	20 mM	0.1583 mL	0.7916 mL	1.5833 mL	3.9582 mL
	25 mM	0.1267 mL	0.6333 mL	1.2666 mL	3.1666 mL
	30 mM	0.1056 mL	0.5278 mL	1.0555 mL	2.6388 mL

CGP 12177 hydrochloride Related Classifications

Metabolic Disease Cardiovascular Disease

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.

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CGP 12177 hydrochloride (Synonyms: (±)-CGP 12177 hydrochloride)

Other Forms of CGP 12177 hydrochloride:

CGP 12177 hydrochloride Related Antibodies

Featured Recommendations

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View All Adrenergic Receptor Isoform Specific Products:

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References

Customer Review

CGP 12177 hydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

CGP 12177 hydrochloride Related Classifications

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