ZP3022
Based on 1 publication(s) in Google Scholar
ZP3022 is a dual GLP-1R/CCK-2R agonist. ZP3022 enhances insulin secretion, improves glycemic control and glucose tolerance, lowers blood glucose and HbA1c levels, reduces food intake and body weight, and inhibits gastric emptying. ZP3022 does not activate CCK-1R. ZP3022 can be used in research on diabetes and obesity.
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- Purity : 98.00%
- CAS No.: 1345835-12-2
- 화학식: C199H294N48O61S
- 분자량:4366.81
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보관:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ZP3022
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Biological Activity
제품 설명
IC50 & Target
[1]|
GLP-1 |
CCKBR |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.069 nM
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Activation of human GLP-1R in HEK293 cells assessed as cAMP accumulation incubated 20 min at 37 °C.
Activation of human GLP-1R in HEK293 cells assessed as cAMP accumulation incubated 20 min at 37 °C.
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33125843 |
| HEK293 | EC50 |
9.9 nM
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Activation of human CCK-2R in HEK293 cells assessed as pERK1/2 by AlphaScreen SureFire ERK 1/2 assay incubated 5 min at room temperature.
Activation of human CCK-2R in HEK293 cells assessed as pERK1/2 by AlphaScreen SureFire ERK 1/2 assay incubated 5 min at room temperature.
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33125843 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:INS-1 cells
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Concentration:30 mM glucose (glucotoxicity media)
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Incubation Time:24 h (ZP3022); 5 h (MTT)
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Result:Had a lower cell protective effect at 100 nM than 6a and 6b.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | AUCinf |
|---|---|---|---|---|---|
| Mice[1] | 50 nmol/Kg | s.c. | 1.2 h | 2 h | 9587 ng·h/mL |
In Vivo
ZP3022 (25-100 nmol/kg; s.c.; single injection) lowers blood glucose and reduces food intake in nonfasted db/db mice, but its duration of action and anorectic effect are less than those of 6a and 6b[1].
ZP3022 (25 nmol/kg; s.c.; three times daily for 21 days) improves glycemic control and islet morphology in db/db mice, but less than 6a and 6b[1].
ZP3022 (25 nmol/kg; s.c.; three times daily for 42 days followed by saline washout for 42 days) produces long-lasting improvements in glucose tolerance and HbA1c in db/db mice over a 12-week study[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BKS-Leprdb/Nju (male, 8 weeks, db/db)[1]
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Dosage:25 nmol/kg
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Administration:i.p.; single injection 30 min before glucose loading
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Result:Showed less glucose-lowering activity than 6a and 6b.
Enhanced plasma insulin levels were observed in db/db mice; insulinotropic activity was lower than that of 6a and 6b.
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Animal Model:BKS-Leprdb/Nju (male, 8 weeks, db/db)[1]
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Dosage:25 and 100 nmol/kg
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Administration:s.c.; single injection
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Result:The glucose-lowering duration of 6a and 6b was longer than that of liraglutide, independent of dose; the blood glucose nadir in 6a- and 6b-treated groups was lower than in liraglutide-treated groups.
Reduced food intake, but 6a and 6b exhibited better anorectic effects than liraglutide.
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Animal Model:BKS-Leprdb/Nju (male, 9 weeks, db/db)[1]
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Dosage:25 nmol/kg
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Administration:s.c.; three times daily for 21 days
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Result:6a and 6b caused more profound reductions in cumulated food intake and body weight gain than liraglutide.
Improved fasted blood glucose and HbA1c, but the effects were less than those of 6a and 6b.
Increased islet areas and numbers were observed in mice; 6a and 6b increased % β-cell area per islet.
Decreased % non-β-cell (α-cell) area similarly to 6a and 6b.
Insulin IOD increased after 6a or 6b administration, larger than after liraglutide administration.
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Animal Model:BKS-Leprdb/Nju (male, 8 weeks, db/db)[1]
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Dosage:25 nmol/kg
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Administration:s.c.; three times daily for 42 days; saline washout for 42 days
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Result:Mice showed prominent improvements in glucose tolerance, with higher OGTT AUC values than 6a and 6b groups.
Reduced HbA1c values measured on day 43 and day 85.
The improvements in glucose tolerance and fasted blood glucose were less evident than those in 6a and 6b groups.
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Animal Model:C57BL/6 (male, ~6 months)[1]
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Dosage:25 nmol/kg
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Administration:s.c.; three times daily for 21 days
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Result:Decreased body weight by ∼17.8% and body fat content by ∼24.5%.
6a and 6b caused greater body weight and fat mass reductions than liraglutide.
6a and 6b also exhibited more profound effects on reducing food intake, lowering fasting blood glucose, improving glucose tolerance, and regulating serum lipids than liraglutide.
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Animal Model:ICR (male, 20-25 g)[1]
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Dosage:25 nmol/kg
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Administration:i.p.; single injection
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Result:Inhibited gastric emptying, but the effects of 6a and 6b on gastric emptying were better than those of liraglutide.
Chemical Information
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CAS No. 1345835-12-2
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Appearance Solid
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분자량 4366.81
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화학식 C199H294N48O61S
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Color White to off-white
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Sequence
His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-(8Ado)-(8Ado)-Tyr-Gly-Trp-Leu-Asp-Phe-NH2 8Ado: 8-amino-3,6-dioxaoctanoic acid
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Sequence Shortening
HGEGTFTSDLSKQMEEEAVRLFIEWLKN-(8Ado)-(8Ado)-YGWLDF-NH2 8Ado: 8-amino-3,6-dioxaoctanoic acid
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
In Vitro:
DMSO : 100 mg/mL (22.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (304 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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, 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 | 0.2290 mL | 1.1450 mL | 2.2900 mL | 5.7250 mL |
| 5 mM | 0.0458 mL | 0.2290 mL | 0.4580 mL | 1.1450 mL | |
| 10 mM | 0.0229 mL | 0.1145 mL | 0.2290 mL | 0.5725 mL | |
| 15 mM | 0.0153 mL | 0.0763 mL | 0.1527 mL | 0.3817 mL | |
| 20 mM | 0.0115 mL | 0.0573 mL | 0.1145 mL | 0.2863 mL |
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