GLP-1R/GIPR agonist-1 (soduim)

Name: GLP-1R/GIPR agonist-1 (soduim)
Brand: MedChemExpress
SKU: HY-P10302A
Rating: 4.5 (0 reviews)

製品番号: HY-P10302A 純度: 98.24%: Data Sheet SDS COA 取扱説明書
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GLP-1R/GIPR agonist-1 sodium is a dual GLP-1/GIP receptor agonist, with an EC₅₀ of 0.57 nM for GLP-1R and an EC₅₀ of 0.75 nM for GIPR. GLP-1R/GIPR agonist-1 sodium reduces food intake, inhibits weight gain, repairs islet damage, improves glucose tolerance, regulates serum lipid and liver enzyme levels, ameliorates hepatic vacuolization, reduces hepatic fat accumulation, delays the progression of hepatic fibrosis, and exhibits long-lasting hypoglycemic activity. GLP-1R/GIPR agonist-1 sodium can be used in research related to type 2 diabetes, obesity, and non-alcoholic steatohepatitis.

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GLP-1R/GIPR agonist-1 (soduim) 構造式

容量	価格（税別）	在庫状況	数量
1 mg	$115	在庫あり	Estimated Time of Arrival: December 31
5 mg	$290	在庫あり	Estimated Time of Arrival: December 31
10 mg	$465	在庫あり	Estimated Time of Arrival: December 31
25 mg	$860	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1290	在庫あり	Estimated Time of Arrival: December 31
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200 mg		お問い合わせ

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製品説明

IC₅₀ & Target

EC₅₀: 0.57 nM (GLP-1R), 0.75 nM (GIPR)

体外実験

GLP-1R/GIPR agonist-1 sodium (CY-5) is a dual GLP-1R/GIPR agonist without GCGR activity, with an EC₅₀ of 0.57 nM for activating GLP-1R and an EC₅₀ of 0.75 nM for activating GIPR in overexpressed HEK-293 cells^[1].

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

体内実験

GLP-1R/GIPR agonist-1 sodium (30 nM/kg, i.p.; single dose) exerts long-lasting hypoglycemic activity in normal ICR mice, with a duration of action comparable to that of Semaglutide (HY-114118)^[1].
GLP-1R/GIPR agonist-1 sodium (30 nM/kg; i.p.; single dose '; daily administration; 32 days (chronic)) achieves acute glycemic stabilization effects comparable to those of Semaglutide in type 2 diabetic mice, and chronic administration significantly reduces food/water intake, suppresses body weight gain, and repairs islet damage^[1].
GLP-1R/GIPR agonist-1 sodium (30 nM/kg; i.p.; daily; for 4 consecutive weeks (chronic); single administration ') exerts potent acute appetite-suppressive effects in DIO mice, and also reduces long-term food/water intake, decreases body weight gain, and achieves stable blood glucose control^[1].
GLP-1R/GIPR agonist-1 sodium (30 nM/kg; i.p.; single dose) effectively promotes insulin secretion and stabilizes blood glucose in normal SD rats^[1].
GLP-1R/GIPR agonist-1 sodium (30 nM/kg; s.c.; single administration) exerts hypoglycemic activity for 34 h in non-fasted ob/ob mice and significantly reduces their body weight^[1].
GLP-1R/GIPR agonist-1 sodium (30 nM/kg; i.p.; daily; for 4 consecutive weeks) significantly improves lipid metabolism, reduces liver enzyme levels, and prevents liver injury in NASH mice^[1].

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

Animal Model:	ICR mice (male, 10 weeks old, 18-22 g)^[1]
Dosage:	30 nM/kg
Administration:	i.p.; single dose
Result:	Exhibited hypoglycemic efficacy duration equivalent to semaglutide. Maintained blood glucose stabilization through repeated glucose tolerance testing cycles.

Animal Model:	ICR mice (male, 10 weeks old, 18-22 g, intraperitoneal injection of 40 mg/kg STZ (HY-13753) followed by 1 week of feeding, fasting blood glucose >11.1 mmol/L, random blood glucose >16.7 mmol/L)^[1]
Dosage:	30 nM/kg
Administration:	i.p.; single dose (acute testing); daily; 32 days (chronic testing)
Result:	Achieved blood glucose stabilization time and glucose reduction percentage equivalent to semaglutide in acute testing. Suppressed daily and cumulative food/water intake to levels equivalent to semaglutide in chronic treatment. Significantly inhibited body weight gain (with better weight reduction than CY-16). Reduced pancreatic islet inflammation, preserved islet cell structure, and repaired islet damage in chronic treatment.

Animal Model:	C57BL/6 mice (male, 10 weeks old, 18-22 g, fed high-fat diet for 8 weeks, body weight >20% more than normal diet-fed controls)^[1]
Dosage:	30 nM/kg
Administration:	i.p.; daily; 4 weeks (chronic testing); single dose (acute appetite suppression testing)
Result:	Suppressed cumulative food/water intake to levels equivalent to semaglutide in chronic treatment. Inhibited body weight gain more effectively than E1 in chronic treatment. Maintained stable fasting blood glucose levels in chronic treatment. Resulted in near-zero food intake in the first 8 h post-administration in acute treatment, with cumulative food intake equivalent to semaglutide. Preserved pancreatic islet structure in chronic treatment.

Animal Model:	SD rats (male, 5-6 weeks old, 180-220 g)^[1]
Dosage:	30 nM/kg
Administration:	i.p.; single dose
Result:	Significantly promoted insulin secretion (with insulin AUC_0-180ₘᵢₙ equivalent to semaglutide). Reduced blood glucose AUC_0-180ₘᵢₙ compared to saline controls. Stabilized blood glucose levels post-administration, with no sharp peak observed in the saline group.

Animal Model:	B6.v-Lepob/J (ob/ob) mice (6-7 weeks old, half male/half female)^[1]
Dosage:	30 nM/kg
Administration:	s.c.; single dose
Result:	Significantly decreased blood glucose starting 2 h post-administration, with hypoglycemic duration lasting 34 h. Reduced body weight by 2.0 g at 24 h, 0.9 g at 48 h, and 0.1 g at 72 h post-administration, which was significantly lower than the control group and equivalent to semaglutide.

Animal Model:	C57BL/6 mice (male, fed NASH-inducing diet [40% fat, 40% carbohydrates, 2% cholesterol] for 8 weeks)^[1]
Dosage:	30 nM/kg
Administration:	i.p.; daily; 4 weeks
Result:	Significantly reduced serum TG, TC, LDL-C, AST, and ALT levels compared to saline controls. Significantly increased serum HDL-C levels compared to saline controls. Showed significant improvement in hepatocyte inflammation, reduced lipid droplets, and improved liver vacuolation compared to the saline group, with better liver protection than semaglutide.

分子量

4861.38 (free base)

分子式

C₂₂₀H₃₃₄N₅₅O₆₉.xNa

Appearance

Solid

Color

White to off-white

Sequence

His-{Aib}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-{Aib}-Leu-Asp-Lys-Arg-Ala-Ala-Lys(AEEA-AEEA-gammaGlu-C18 diacid)-Asp-Phe-Val-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

Sequence Shortening

H-{Aib}-QGTFTSDYSK-{Aib}-LDKRAA-K(AEEA-AEEA-gammaGlu-C18 diacid)-DFVEWLKNGGPSSGAPPPS-NH2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Sealed storage, away from moisture
Powder	-80°C	2 years
	-20°C	1 year
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

H₂O : ≥ 100 mg/mL

*"≥" means soluble, but saturation unknown.

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

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一般には略語で表示されます：C₁V₁ = C₂V₂

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

純度とドキュメンテーション

純度: 98.24%

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データシート (301 KB) SDS (252 KB)

COA (274 KB) RP-HPLC (254 KB) MS (73 KB) Elemental Analysis Report (133 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Liu C, et al. Discovery of a novel GLP-1/GIP dual receptor agonist CY-5 as long-acting hypoglycemic, anti-obesity agent. Bioorg Chem. 2021 Jan;106:104492. [Content Brief]