KwFwLL-NH2
KwFwLL-NH2, a hexapeptide, is a ghrelin receptor ligand. KwFwLL-NH2 can act as a specific inverse agonist at the ghrelin receptor but with moderate potency (EC50=45.6 nM).
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- CAS. Nr.: 942266-38-8
- Formel: C49H66N10O6
- Molecular Weight:891.11
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
>1000 nM
Compound: KwFwLL-NH2
|
Agonist activity at human ghrelin receptor Asp2:20Lys(Asp99) mutant expressed in african green monkey COS7 cells assessed as inhibition of inositol phosphate accumulation
Agonist activity at human ghrelin receptor Asp2:20Lys(Asp99) mutant expressed in african green monkey COS7 cells assessed as inhibition of inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
>1000 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Arg6:20Gln(Arg283) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Arg6:20Gln(Arg283) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
>1000 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Gln3:05Ala(Gln120) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Gln3:05Ala(Gln120) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
>1000 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Glu3:09Gln(Glu124) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Glu3:09Gln(Glu124) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
>1000 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Phe7:06Leu(Phe306) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Phe7:06Leu(Phe306) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
>1000 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Phe7:09Ala(Phe312) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Phe7:09Ala(Phe312) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
13 nM
Compound: KwFwLL-NH2
|
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
|
[PMID: 17371869] |
| COS-7 | IC50 |
19 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
2.6 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
21 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
27 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
29 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
32 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
36 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
43 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
60 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
61 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
83 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
Inverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
|
[PMID: 17371869] |
| COS-7 | IC50 |
>1000 nM
Compound: KwFwLL-NH2
|
Agonist activity at human ghrelin receptor Asp2:20Asn(Asp99) mutant expressed in african green monkey COS7 cells assessed as inhibition of inositol phosphate accumulation
Agonist activity at human ghrelin receptor Asp2:20Asn(Asp99) mutant expressed in african green monkey COS7 cells assessed as inhibition of inositol phosphate accumulation
|
[PMID: 17371869] |
| HEK-293T | EC50 |
100 nM
Compound: KwFwLL-NH2
|
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
|
[PMID: 27072910] |
Chemical Information
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CAS. Nr. 942266-38-8
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Molecular Weight 891.11
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Formel C49H66N10O6
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SMILES
O=C(N[C@H](CC1=CNC2=CC=CC=C12)C(N[C@@H](CC3=CC=CC=C3)C(N[C@H](CC4=CNC5=CC=CC=C45)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N)=O)=O)=O)=O)=O)[C@H](CCCCN)N
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Sequence
Lys-{D-Trp}-Phe-{D-Trp}-Leu-Leu-NH2
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Sequence Shortening
K-{D-Trp}-F-{D-Trp}-LL-NH2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)