1. GPCR/G Protein
  2. GHSR
  3. 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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KwFwLL-NH2

KwFwLL-NH2 Chemical Structure

CAS No. : 942266-38-8

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Description

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)[1].

Cellular Effect
Cell Line Type Value Description References
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]
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]
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]
Molecular Weight

891.11

Formula

C49H66N10O6

CAS No.
Sequence

Lys-{D-Trp}-Phe-{D-Trp}-Leu-Leu-NH2

Sequence Shortening

K-{D-Trp}-F-{D-Trp}-LL-NH2

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Product Name:
KwFwLL-NH2
Cat. No.:
HY-P10673
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