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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 1 mg/ml in 30% acetonitrile / water

Preparing Stock Solutions

The following data is based on the product molecular weight 1299.56. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.77 mL 3.85 mL 7.69 mL
5 mM 0.15 mL 0.77 mL 1.54 mL
10 mM 0.08 mL 0.38 mL 0.77 mL
50 mM 0.02 mL 0.08 mL 0.15 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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: MEN11270 analog icatibant HOE 140 HOE140 b2 bradykinin receptor antagonist Bradykinin Receptors

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