A cyclic peptide and negative allosteric modulator of TrkB
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Cyclotraxin B

Item No. 42991

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cyclic (1→11)-disulfide L-cysteinyl-L-asparaginyl-L-prolyl-L-methionylglycyl-L-tyrosyl-L-threonyl-L-lysyl-L-α-glutamylglycyl-L-cysteine
CAS Number
1203586-72-4
Molecular Formula
C48H73N13O17S3
Formula Weight
1200.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlPBS (pH 7.2): Soluble: ≥ 10 mg/ml
SMILES
O=C1N2[C@](CCC2)([H])C(N[C@H](C(NCC(N[C@H](C(N[C@@](C(N[C@H](C(N[C@H](C(NCC(N[C@@H](CSSC[C@@H](C(N[C@H]1CC(N)=O)=O)N)C(O)=O)=O)=O)CCC(O)=O)=O)CCCCN)=O)([H])[C@H](O)C)=O)CC3=CC=C(C=C3)O)=O)=O)CCSC)=O
InChi Code
InChI=1S/C48H73N13O17S3/c1-24(62)39-46(75)58-28(6-3-4-15-49)43(72)56-29(12-13-38(67)68)41(70)52-21-37(66)55-33(48(77)78)23-81-80-22-27(50)40(69)59-32(19-35(51)64)47(76)61-16-5-7-34(61)45(74)57-30(14-17-79-2)42(71)53-20-36(65)54-31(44(73)60-39)18-25-8-10-26(63)11-9-25/h8-11,24,27-34,39,62-63H,3-7,12-23,49-50H2,1-2H3,(H2,51,64)(H,52,70)(H,53,71)(H,54,65)(H,55,66)(H,56,72)(H,57,74)(H,58,75)(H,59,69)(H,60,73)(H,67,68)(H,77,78)/t24-,27+,28+,29+,30+,31+,32+,33+,34+,39+/m1/s1
InChi Key
JLBMMJHZUYBFGX-ZHTCEXBHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    Cyclotraxin B is a cyclic peptide and negative allosteric modulator of tropomysin-related kinase B (TrkB).1 It inhibits BDNF-induced TrkB activity in a kinase receptor activation ELISA (KIRA-ELISA) using tetracycline-responsive CHO-K1 cells expressing recombinant human TrkB (TetOn-rhTrkB cells; IC50 = 0.3 nM). It also inhibits BDNF-induced neurite outgrowth in nerve growth factor (NGF) non-responding mutant PC12 cells expressing TrkB (nnr5 PC12-TrkB cells; IC50 = 12.2 pM). Cyclotraxin B (20 mg/kg per day) reduces mechanical, but not thermal, allodynia in the ipsilateral and contralateral paw in a rat model of thermal injury exacerbated by chronic intermittent stress.2 Intravenous administration of cyclotraxin B fused to HIV-1 Tat protein, which increases brain delivery, increases the number of entries into and the ratio of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cazorla, M., Jouvenceau, A., Rose, C., et al. Cyclotraxin-B, the first highly potent and selective TrkB inhibitor, has anxiolytic properties in mice. PLoS One 5(3), e9777 (2010).

    2. Sosanya, N.M., Garza, T.H., Stacey, W., et al. Involvement of brain-derived neurotrophic factor (BDNF) in chronic intermittent stress-induced enhanced mechanical allodynia in a rat model of burn pain. BMC Neurosci. 20(1), 17 (2019).