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Art. -Nr.: HY-P12402

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NN9056

NN9056 is a selective CCK-1 receptor agonist. NN9056 has an IC₅₀ value of 0.105 nM for the human target and an IC₅₀ value of 0.123 nM for the porcine target. NN9056 inhibits food intake and induces body weight loss. NN9056 improves insulin (Insulin (human)) (HY-P0035) sensitivity secondary to body weight reduction. NN9056 is a long-acting analog with an extended plasma half-life that provides all-day plasma exposure coverage. NN9056 can be used for obesity research.

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CAS. Nr.: 2064085-67-0
Formel: C₈₉H₁₃₃N₁₃O₂₇S
Molecular Weight:1849.14

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (290 KB)

NN9056 Chemical Structure

CAS. Nr.: 2064085-67-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Cholecystokinin Receptor Isoform-spezifische Produkte anzeigen :

CCKAR
CCKBR

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	EC50	0.205 nM	Activation of overexpressed pig CCK-1 receptors in COS-7 cells assessed by IP-One HTRF assay measuring IP1 accumulation. Activation of overexpressed pig CCK-1 receptors in COS-7 cells assessed by IP-One HTRF assay measuring IP1 accumulation.	31175319
COS-7	EC50	0.093 nM	Activation of overexpressed human CCK-1 receptors in COS-7 cells assessed by IP-One HTRF assay measuring IP1 accumulation. Activation of overexpressed human CCK-1 receptors in COS-7 cells assessed by IP-One HTRF assay measuring IP1 accumulation.	31175319

In Vitro

NN9056 binds COS-7-expressed pig and human CCK-1 receptors with IC₅₀ values of 0.123 nM and 0.105 nM, respectively^[1].
NN9056 activates COS-7-expressed pig and human CCK-1 receptors with EC₅₀ values of 0.205 nM and 0.093 nM, respectively^[1].

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

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC	T_1/2
Pig^[1]	5 nmol/Kg	s.c.	3.4 h	76.775 nM	3091 kg·h/L	128 h

In Vivo

Carbohydrate MetabolismLipid MetabolismOthers

Carbohydrate Metabolism

Lipid Metabolism

NN9056 (2-10 nmol/kg; s.c.; once daily; 13 weeks) reduces food intake and body weight in obese Göttingen Minipigs^[1].

Others

NN9056 (10-100 nmol/kg; s.c.; single administration) reduces feed intake in lean LYD pigs at a dose of 100 nmol/kg, with a smaller reduction at a dose of 10 nmol/kg^[1].
NN9056 (10-80 nmol/kg; s.c.; single administration) dose-dependently reduces feed intake in lean LYD pigs^[1].

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

Animal Model:

Landrace × Yorkshire × Duroc (LYD) (female, approximately 3 months old, 30-35 kg)^[1]
Dosage:

10 nmol/kg and 100 nmol/kg
Administration:

s.c.; single dose
Result:

Food intake was 86% of vehicle from 0-24 h (corresponding to -1.1 kg) and 75% of vehicle from 25-48 h (corresponding to -0.8 kg).
At 10 nmol/kg, food intake was not significantly reduced and was 22% lower than vehicle from 0-24 h (corresponding to -0.3 kg) and 33% lower from 25-48 h (corresponding to -0.4 kg).

Animal Model:

Landrace × Yorkshire × Duroc (LYD) (female, approximately 3 months old, 30-35 kg)^[1]
Dosage:

10 nmol/kg; 20 nmol/kg; 40 nmol/kg; 80 nmol/kg
Administration:

s.c.; single dose
Result:

Food intake was dose-dependently reduced after a single s.c. dose of 10, 20, 40, or 80 nmol/kg.
At 20 and 40 nmol/kg, food intake was significantly reduced for 2 days, and at 80 nmol/kg, food intake was significantly reduced for at least 4 days.

Animal Model:

Göttingen Minipig (female, ovariectomised, approximately 18 months old at study start)^[1]
Dosage:

low dose: initially 5 nmol/kg, then 3 nmol/kg, then 2 nmol/kg; high dose: 10 nmol/kg
Administration:

s.c.; once daily; 13 weeks; 3-week wash-out
Result:

Accumulated food intake from days 1-77 was 51.5 kg in the low-dose group and 41.8 kg in the high-dose group.
Body weight change from days 1-77 was -2.3% in the low-dose group and -7.2% in the high-dose group.
During IVGTT, glucose clearance (K_G) was 4.1 min^-1 in the low-dose group and 3.4 min^-1 in the high-dose group; AUC_insulin was 48.9 nM·min in the low-dose group and 52.0 nM·min in the high-dose group.
Fasting plasma parameters were: low dose-glucose 4.0 mM, insulin 78 pM, C-peptide 24 pM, glucagon 13.5 pM, total GLP-1 37.1 pM, TBA 7.8 µM, TG 0.56 mM, TC 2.1 mM, leptin 38.6 ng/mL HE, α-amylase 1568 U/L, lipase 12.5 U/L; high dose-glucose 4.0 mM, insulin 68 pM, C-peptide 24 pM, glucagon 11.6 pM, total GLP-1 37.6 pM, TBA 9.0 µM, TG 0.41 mM, TC 2.1 mM, leptin 47.2 ng/mL HE, α-amylase 1755 U/L, lipase 9.4 U/L.

Related Protocols :

Chemical Information

CAS. Nr. 2064085-67-0
Molecular Weight 1849.14
Formel C₈₉H₁₃₃N₁₃O₂₇S
SMILES

NC([C@H](CC1=CC=CC=C1)N(C)C([C@@H](CC(O)=O)N(C)C([C@H](CCCC)NC([C@@H](NC(CNC([C@H](CCCC)NC([C@@H](NC([C@H](CC(O)=O)NC(COCCOCCNC(COCCOCCNC(CC[C@H](NC(CCCCCCCCCCCCCCCCC(O)=O)=O)C(O)=O)=O)=O)=O)=O)CC2=CC=C(C=C2)CS(=O)(O)=O)=O)=O)=O)CC3=CNC4=CC=CC=C34)=O)=O)=O)=O
Sequence

Asp(AEEA-AEEA-γGlu-C18 diacid)-Phe(4-sulfomethyl)-Nle-Gly-Trp-Nle-DAsp(NMe)-Phe-NH2
Sequence Shortening

Asp(AEEA-AEEA-γGlu-C18 diacid)-Phe(4-sulfomethyl)-Nle-GW-Nle-DAsp(NMe)-F-NH2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Christoffersen BØ, et al. Long-acting CCK analogue NN9056 lowers food intake and body weight in obese Göttingen Minipigs. International journal of obesity (2005). 2020 Feb;44(2):447-456.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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