MEN 11270

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Cat.No. 3978 - MEN 11270 | D-Arg-Arg-Pro-Hyp-Gly-Thi-cyclo(7γ-10α)-(Dab-D-Tic-Oic-Arg) | CAS No. 235082-52-7
Description: Selective B2 antagonist; analog of HOE 140 (Cat. No. 3014)
Datasheet
Citations
Reviews
Literature

Biological Activity

Peptide antagonist of the B2 bradykinin receptor (pKi = 10.3); conformationally constrained cyclized analog of HOE 140 (Cat. No. 3014). Blocks hypotension and bronchoconstriction in vivo. Displays selectivity for B2 over 29 other receptors and ion channels (pIC50 < 5.5).

Technical Data

M. Wt 1299.56
Formula C60H90N20O11S
Sequence RRPXGXXXXR

(Modifications: Arg-1 = D-Arg, X-1 = Hyp, X-2 = Thi, X-3 = Dab, X-4 = D-Tic, X-5 = Oic, cyclized 7γ - 10α)

Storage Store at -20°C
CAS Number 235082-52-7
PubChem ID 90488898
InChI Key LPLBKEKLEUYDEJ-UUHVOKIZSA-N
Smiles [H]N[C@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N1C[C@H](O)C[C@H]1C(=O)NCC(=O)N[C@H](CC1=CC=CS1)C(=O)N[C@H]1CCNC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]2CC3CCCCC3N2C(=O)[C@H]2CC3=CC=CC=C3CN2C1=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solubility Soluble to 1 mg/ml in 30% acetonitrile / water

References

References are publications that support the biological activity of the product.

Meini et al (1999) MEN 11270, a novel selective constrained peptide antagonist with high affinity at the human B2 kinin receptor. J.Pharmacol.Exp.Ther. 289 1250 PMID: 10336513

Tramontana et al (2001) Differences between peptide and nonpeptide B2 bradykinin receptor antagonists in blocking bronchoconstriction and hypotension induced by bradykinin in anesthetized guinea pigs J.Pharmacol.Exp.Ther. 296 1051 PMID: 11181940

Cucchi et al (2002) Interaction of linear and cyclic peptide antagonists at the human B(2) kinin receptor. Peptides 23 1457 PMID: 12182947


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Keywords: MEN 11270, MEN 11270 supplier, MEN11270, analog, icatibant, HOE, 140, HOE140, b2, bradykinin, receptor, antagonist, Bradykinin, Receptors, 3978, Tocris Bioscience

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