An inhibitor of the Cav2.2-CRMP2 protein-protein interaction
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Tat-CBD3 (trifluoroacetate salt)

Item No. 37448

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Molecular Formula
C134H243N59O32 • XCF3COOH
Formula Weight
3192.7
Purity
≥95%
Formulation (Request formulation change)
A solid
Peptide Sequence
YGRKKRRQRRRARSRLAELRGVPRGL-OH
Solubility(Learn about Variance in Solubility)
Water: Soluble
SMILES
OC(C(F)(F)F)=O.O=C(NCC(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN[H])C(N[C@@H](CCCCN[H])C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CO)C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N[C@H](C(N[C@@H](CCC(O)=O)C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(NCC(N[C@@H](C(C)C)C(N1CCC[C@H]1C(N[C@@H](CCCNC(N)=N)C(NCC(N[C@H](C(O)=O)CC(C)C)=O)=O)=O)=O)=O)=O)=O)CC(C)C)=O)=O)C)=O)CC(C)C)=O)=O)=O)=O)C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC2=CC=C(O)C=C2)N[H]
InChi Code
InChI=1S/C134H243N59O32.C2HF3O2/c1-68(2)60-91(119(219)173-73(10)103(203)177-90(44-46-100(200)201)118(218)190-92(61-69(3)4)120(220)178-77(28-15-49-159-125(139)140)105(205)171-66-99(199)192-101(71(7)8)123(223)193-59-25-38-95(193)122(222)188-78(29-16-50-160-126(141)142)106(206)170-65-98(198)175-93(124(224)225)62-70(5)6)189-115(215)88(37-24-58-168-134(157)158)186-121(221)94(67-194)191-116(216)83(32-19-53-163-129(147)148)176-102(202)72(9)172-107(207)82(31-18-52-162-128(145)146)181-111(211)84(33-20-54-164-130(149)150)183-113(213)86(35-22-56-166-132(153)154)185-117(217)89(43-45-96(138)196)187-114(214)87(36-23-57-167-133(155)156)184-112(212)85(34-21-55-165-131(151)152)182-110(210)81(27-12-14-48-136)180-109(209)80(26-11-13-47-135)179-108(208)79(30-17-51-161-127(143)144)174-97(197)64-169-104(204)76(137)63-74-39-41-75(195)42-40-74;3-2(4,5)1(6)7/h39-42,68-73,76-95,101,194-195H,11-38,43-67,135-137H2,1-10H3,(H2,138,196)(H,169,204)(H,170,206)(H,171,205)(H,172,207)(H,173,219)(H,174,197)(H,175,198)(H,176,202)(H,177,203)(H,178,220)(H,179,208)(H,180,209)(H,181,211)(H,182,210)(H,183,213)(H,184,212)(H,185,217)(H,186,221)(H,187,214)(H,188,222)(H,189,215)(H,190,218)(H,191,216)(H,192,199)(H,200,201)(H,224,225)(H4,139,140,159)(H4,141,142,160)(H4,143,144,161)(H4,145,146,162)(H4,147,148,163)(H4,149,150,164)(H4,151,152,165)(H4,153,154,166)(H4,155,156,167)(H4,157,158,168);(H,6,7)/t72-,73-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,101-;/m0./s1
InChi Key
HTJTYNLPRSFEKI-YSLRCEGOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $31

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    5 mg

    $147

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    10 mg

    $278

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    25 mg

    $616

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    Product Description

    Tat-CBD3 is an inhibitor of the protein-protein interaction between the N-type voltage-gated calcium channel Cav2.2 and collapsin response mediator protein 2 (CRMP2).1,2 It also inhibits the protein-protein interaction between CRMP2 and the NMDA receptor NR2B subunit.3 Tat-CBD3 (10 µM) inhibits the Cav2.2-CRMP2 interaction by 43% in a cell-free assay and the NMDA receptor NR2B subunit-CRMP2 interaction in an immunoprecipitation assay.2,3 It reduces voltage-induced calcium currents by approximately 60% in primary rat dorsal root ganglion (DRG) neurons and glutamate-induced increases in cytosolic calcium levels in primary rat hippocampal neurons.1,3 Tat-CBD3 (20 mg/kg) decreases infarct volume in a rat model of cerebral ischemia induced by middle cerebral artery occlusion (MCAO).4 Intrathecal administration of Tat-CBD3 (20 µg/5 µl) prevents carrageenan-induced thermal hypersensitivity in rats.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brittain, J.M., Duarte, D.B., Wilson, S.M., et al. Suppression of inflammatory and neuropathic pain by uncoupling CRMP-2 from the presynaptic Ca²⁺ channel complex. Nat. Med. 17(7), 822-829 (2011).

    2. François-Moutal, L., Wang, Y., Moutal, A., et al. A membrane-delimited N-myristoylated CRMP2 peptide aptamer inhibits CaV2.2 trafficking and reverses inflammatory and postoperative pain behaviors. Pain 156(7), 1247-1264 (2015).

    3. Brustovetsky, T., Pellman, J.J., Yang, X.F., et al. Collapsin response mediator protein 2 (CRMP2) interacts with N-methyl-D-aspartate (NMDA) receptor and Na+/Ca2+ exchanger and regulates their functional activity. The Journal of Biological Chemisty 289(11), 7470-7482 (2014).

    4. Brittain, J.M., Pan, R., You, H., et al. Disruption of NMDAR-CRMP-2 signaling protects against focal cerebral ischemic damage in the rat middle cerebral artery occlusion model. Channels (Austin) 6(1), 52-59 (2012).