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Cortistatin-29 (rat) (trifluoroacetate salt)

Basic information Safety Supplier Related

Cortistatin-29 (rat) (trifluoroacetate salt) Basic information

Product Name:
Cortistatin-29 (rat) (trifluoroacetate salt)
Synonyms:
  • Cortistatin-29 (rat) (trifluoroacetate salt)
  • Cortistatin-29 (rat) (H-6444.0500)
  • L-Lysine, 5-oxo-L-prolyl-L-α-glutamyl-L-arginyl-L-prolyl-L-prolyl-L-leucyl-L-glutaminyl-L-glutaminyl-L-prolyl-L-prolyl-L-histidyl-L-arginyl-L-α-aspartyl-L-lysyl-L-lysyl-L-prolyl-L-cysteinyl-L-lysyl-L-asparaginyl-L-phenylalanyl-L-phenylalanyl-L-tryptophyl-L-lysyl-L-threonyl-L-phenylalanyl-L-seryl-L-s...
CAS:
1815618-17-7
MF:
C161H240N46O41S2
MW:
3540.04
Mol File:
1815618-17-7.mol
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Cortistatin-29 (rat) (trifluoroacetate salt) Chemical Properties

Density 
1.54±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
Water: 1 mg/ml
form 
A lyophilized powder
Sequence
Pyr-Glu-Arg-Pro-Pro-Leu-Gln-Gln-Pro-Pro-His-Arg-Asp-Lys-Lys-Pro-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Ser-Ser-Cys-Lys-OH (Disulfide bonds)
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Cortistatin-29 (rat) (trifluoroacetate salt) Usage And Synthesis

Description

Cortistatin-29 is a neuropeptide that is structurally similar to somatostatin-28. It is produced by cleavage of preprocortistatin to procortistatin, which is cleaved at dibasic amino acids to form cortistatin-29 and cortistatin-14 as well as other partial cleavage products. Cortistatin mRNA is expressed in the human brain and in interneurons of the rat hippocampus and cerebral cortex. Cortistatin-29 binds to somatostatin (SST) receptors with IC50 values of 2.8, 7.1, 0.2, 3, and 13.7 nM for SST1-5, respectively. Cortistatin-29 is found at similar levels as cortistatin-14 in mouse AtT20 cells but is secreted at a lower level. Cortistatin-29 corresponds to residues 85-112 of the rat peptide sequence.

Uses

Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects[1][2][3][4].

in vivo

Cortistatin 29 (1-2 μg) alleviates chronic neuropathic pain in mouse[1].
Cortistatin 29 (1 nmol/mouse; i.p.; three times weekly) shows anti-fibrotic effects in mouse[4].

Animal Model:20-24 g body weight, 8-12 weeks-old mice[1]
Dosage:1 μg in 20 μL for s.c.; 2 μg in 200 μL for i.p.; 20 ng in 10 μL for i.t.
Administration:Every other day for 12 days
Result:Ameliorated hyperalgesia and allodynia, regulated the nerve damageinduced hypersensitization of primary nociceptors, inhibited neuroinflammatory responses, and enhanced the production of neurotrophic factors both at the peripheral and central levels.

IC 50

SSTR1: 2.8 nM (IC50); SSTR2: 7.1 nM (IC50); SSTR3: 0.2 nM (IC50); SSTR4: 3.0 nM (IC50); SSTR5: 13.7 nM (IC50)

References

[1] Falo CP, et al. The Neuropeptide Cortistatin Alleviates Neuropathic Pain in Experimental Models of Peripheral Nerve Injury. Pharmaceutics. 2021 Jun 24;13(7):947. DOI:10.3390/pharmaceutics13070947
[2] Baranowska B, et al. Direct effect of cortistatin on GH release from cultured pituitary cells in the rat. Neuro Endocrinol Lett. 2006 Feb-Apr;27(1-2):153-6. PMID:16648801
[3] Spier AD, et al. Cortistatin: a member of the somatostatin neuropeptide family with distinct physiological functions. Brain Res Brain Res Rev. 2000 Sep;33(2-3):228-41. DOI:10.1016/s0165-0173(00)00031-x
[4] Benitez R, et al. Cortistatin regulates fibrosis and myofibroblast activation in experimental hepatotoxic- and cholestatic-induced liver injury. Br J Pharmacol. 2022 May;179(10):2275-2296. DOI:10.1111/bph.15752

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