TAT-GluA2 3Y | CAS# 1404188-93-7 | AMPA Receptor Endocytosis Inhibitor

MedKoo Cat#: 574060 | Name: TAT-GluA2 3Y

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

TAT-GluA2 3Y is an Inhibitor of AMPA receptor endocytosis. Induces increased hind paw withdrawal latencies following thermal and mechanical stimuli in rats. Also exhibits antinociceptive effects in a rat model of neuropathic pain. Rescues pentobarbital-induced memory retrieval deficits in a rat model of learning and memory.

Chemical Structure

TAT-GluA2 3Y

CAS#1404188-93-7

Theoretical Analysis

MedKoo Cat#: 574060

Name: TAT-GluA2 3Y

CAS#: 1404188-93-7

Chemical Formula: C115H185N43O29

Exact Mass: 2632.4323

Molecular Weight: 2634.02

Elemental Analysis: C, 52.44; H, 7.08; N, 22.87; O, 17.61

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 340.00

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Synonym

TAT-GluA2 3Y

IUPAC/Chemical Name

N/A

InChi Key

JRFBJZYZNDUYJM-ZLIURJSSNA-N

InChi Code

InChI=1S/C115H185N43O29/c1-61(2)92(109(187)157-82(95(173)142-60-91(169)170)54-63-26-34-67(160)35-27-63)158-108(186)85(57-87(121)164)156-106(184)83(55-64-28-36-68(161)37-29-64)144-89(166)59-141-94(172)80(41-43-90(167)168)153-99(177)74(17-5-8-46-118)152-107(185)84(56-65-30-38-69(162)39-31-65)155-104(182)79(23-14-52-139-115(132)133)150-101(179)76(20-11-49-136-112(126)127)148-102(180)77(21-12-50-137-113(128)129)151-105(183)81(40-42-86(120)163)154-103(181)78(22-13-51-138-114(130)131)149-100(178)75(19-10-48-135-111(124)125)147-98(176)73(16-4-7-45-117)146-97(175)72(15-3-6-44-116)145-96(174)71(18-9-47-134-110(122)123)143-88(165)58-140-93(171)70(119)53-62-24-32-66(159)33-25-62/h24-39,61,70-85,92,159-162H,3-23,40-60,116-119H2,1-2H3,(H2,120,163)(H2,121,164)(H,140,171)(H,141,172)(H,142,173)(H,143,165)(H,144,166)(H,145,174)(H,146,175)(H,147,176)(H,148,180)(H,149,178)(H,150,179)(H,151,183)(H,152,185)(H,153,177)(H,154,181)(H,155,182)(H,156,184)(H,157,187)(H,158,186)(H,167,168)(H,169,170)(H4,122,123,134)(H4,124,125,135)(H4,126,127,136)(H4,128,129,137)(H4,130,131,138)(H4,132,133,139)/t70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,92-/m0/s1

SMILES Code

[H]N[C@@H](CC1=CC=C(O)C=C1)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)NCC(O)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in Water

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 2,634.02 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Li W, Gong Q, Zhu W, Ali T, Yu ZJ, Li S, Yu X. AMPA receptor potentiation alleviates NLRP3 knockout-induced fear generalization in mice. Biochem Biophys Res Commun. 2024 Aug 30;722:150074. doi: 10.1016/j.bbrc.2024.150074. Epub 2024 May 23. PMID: 38805785. 2: Lu H, Chen S, Nie Q, Xue Q, Fan H, Wang Y, Fan S, Zhu J, Shen H, Li H, Fang Q, Ni J, Chen G. Synaptotagmin-3 interactions with GluA2 mediate brain damage and impair functional recovery in stroke. Cell Rep. 2023 Mar 28;42(3):112233. doi: 10.1016/j.celrep.2023.112233. Epub 2023 Mar 8. PMID: 36892998. 3: Ge Y, Wang YT. Postsynaptic signaling at glutamatergic synapses as therapeutic targets. Curr Opin Neurobiol. 2022 Aug;75:102585. doi: 10.1016/j.conb.2022.102585. Epub 2022 Jun 20. PMID: 35738196. 4: Jiang H, Liu JP, Xi K, Liu LY, Kong LY, Cai J, Cai SQ, Han XY, Song JG, Yang XM, Wan Y, Xing GG. Contribution of AMPA Receptor-Mediated LTD in LA/BLA-CeA Pathway to Comorbid Aversive and Depressive Symptoms in Neuropathic Pain. J Neurosci. 2021 Aug 25;41(34):7278-7299. doi: 10.1523/JNEUROSCI.2678-20.2021. Epub 2021 Jul 16. PMID: 34272314; PMCID: PMC8387122. 5: Ashby DM, Dias C, Aleksandrova LR, Lapish CC, Wang YT, Phillips AG. Disruption of Long-Term Depression Potentiates Latent Inhibition: Key Role for Central Nucleus of the Amygdala. Int J Neuropsychopharmacol. 2021 Jul 23;24(7):580-591. doi: 10.1093/ijnp/pyab011. PMID: 33693669; PMCID: PMC8299826. 6: Ashourpour F, Jafari A, Babaei P. Chronic administration of Tat-GluR23Y ameliorates cognitive dysfunction targeting CREB signaling in rats with amyloid beta neurotoxicity. Metab Brain Dis. 2021 Apr;36(4):701-709. doi: 10.1007/s11011-020-00662-8. Epub 2021 Jan 9. PMID: 33420884. 7: Qin X, Zaki MG, Chen Z, Jakova E, Ming Z, Cayabyab FS. Adenosine Signaling and Clathrin-Mediated Endocytosis of Glutamate AMPA Receptors in Delayed Hypoxic Injury in Rat Hippocampus: Role of Casein Kinase 2. Mol Neurobiol. 2021 May;58(5):1932-1951. doi: 10.1007/s12035-020-02246-0. Epub 2021 Jan 7. PMID: 33415682; PMCID: PMC8018935. 8: Sun X, Wang N, Wang X, Sun L, Li Y, Cui C. AMPA Receptor in Ventromedial Prefrontal Cortex Plays Different Roles in the Recent and Remote Retrieval of Morphine-Associated Memory. Neurochem Res. 2019 Aug;44(8):1939-1949. doi: 10.1007/s11064-019-02827-z. Epub 2019 Jun 17. PMID: 31209728. 9: Madayag AC, Gomez D, Anderson EM, Ingebretson AE, Thomas MJ, Hearing MC. Cell-type and region-specific nucleus accumbens AMPAR plasticity associated with morphine reward, reinstatement, and spontaneous withdrawal. Brain Struct Funct. 2019 Sep;224(7):2311-2324. doi: 10.1007/s00429-019-01903-y. Epub 2019 Jun 14. PMID: 31201496; PMCID: PMC6698404. 10: Benneyworth MA, Hearing MC, Asp AJ, Madayag A, Ingebretson AE, Schmidt CE, Silvis KA, Larson EB, Ebner SR, Thomas MJ. Synaptic Depotentiation and mGluR5 Activity in the Nucleus Accumbens Drive Cocaine-Primed Reinstatement of Place Preference. J Neurosci. 2019 Jun 12;39(24):4785-4796. doi: 10.1523/JNEUROSCI.3020-17.2019. Epub 2019 Apr 4. PMID: 30948476; PMCID: PMC6561685. 11: Yu Y, Huang Z, Dai C, Du Y, Han H, Wang YT, Dong Z. Facilitated AMPAR endocytosis causally contributes to the maternal sleep deprivation-induced impairments of synaptic plasticity and cognition in the offspring rats. Neuropharmacology. 2018 May 1;133:155-162. doi: 10.1016/j.neuropharm.2018.01.030. Epub 2018 Jan 31. PMID: 29378210. 12: Wang W, Tan T, Yu Y, Huang Z, Du Y, Han H, Dong Z. Inhibition of AMPAR endocytosis alleviates pentobarbital-induced spatial memory deficits and synaptic depression. Behav Brain Res. 2018 Feb 26;339:66-72. doi: 10.1016/j.bbr.2017.11.020. Epub 2017 Nov 21. PMID: 29162383. 13: Wu HF, Chen PS, Hsu YT, Lee CW, Wang TF, Chen YJ, Lin HC. D-Cycloserine Ameliorates Autism-Like Deficits by Removing GluA2-Containing AMPA Receptors in a Valproic Acid-Induced Rat Model. Mol Neurobiol. 2018 Jun;55(6):4811-4824. doi: 10.1007/s12035-017-0685-1. Epub 2017 Jul 21. PMID: 28733898. 14: Bhattacharya S, Kimble W, Buabeid M, Bhattacharya D, Bloemer J, Alhowail A, Reed M, Dhanasekaran M, Escobar M, Suppiramaniam V. Altered AMPA receptor expression plays an important role in inducing bidirectional synaptic plasticity during contextual fear memory reconsolidation. Neurobiol Learn Mem. 2017 Mar;139:98-108. doi: 10.1016/j.nlm.2016.12.013. Epub 2016 Dec 27. PMID: 28034784. 15: Chen Z, Stockwell J, Cayabyab FS. Adenosine A1 Receptor-Mediated Endocytosis of AMPA Receptors Contributes to Impairments in Long-Term Potentiation (LTP) in the Middle-Aged Rat Hippocampus. Neurochem Res. 2016 May;41(5):1085-97. doi: 10.1007/s11064-015-1799-3. Epub 2015 Dec 23. PMID: 26700433. 16: Liu TY, Cheng Y, Qin XY, Yu LC. Pharmacologically inhibiting GluR2 internalization alleviates neuropathic pain. Neurosci Bull. 2015 Oct;31(5):611-6. doi: 10.1007/s12264-015-1556-2. Epub 2015 Aug 6. PMID: 26248656; PMCID: PMC5563682. 17: Chen Z, Xiong C, Pancyr C, Stockwell J, Walz W, Cayabyab FS. Prolonged adenosine A1 receptor activation in hypoxia and pial vessel disruption focal cortical ischemia facilitates clathrin-mediated AMPA receptor endocytosis and long-lasting synaptic inhibition in rat hippocampal CA3-CA1 synapses: differential regulation of GluA2 and GluA1 subunits by p38 MAPK and JNK. J Neurosci. 2014 Jul 16;34(29):9621-43. doi: 10.1523/JNEUROSCI.3991-13.2014. PMID: 25031403; PMCID: PMC6608326. 18: Choi FY, Ahn S, Wang YT, Phillips AG. Interference with AMPA receptor endocytosis: effects on behavioural and neurochemical correlates of amphetamine sensitization in male rats. J Psychiatry Neurosci. 2014 May;39(3):189-99. doi: 10.1503/jpn.120257. PMID: 24290077; PMCID: PMC3997604. 19: Dong Z, Bai Y, Wu X, Li H, Gong B, Howland JG, Huang Y, He W, Li T, Wang YT. Hippocampal long-term depression mediates spatial reversal learning in the Morris water maze. Neuropharmacology. 2013 Jan;64:65-73. doi: 10.1016/j.neuropharm.2012.06.027. Epub 2012 Jun 23. PMID: 22732443. 20: Dias C, Wang YT, Phillips AG. Facilitated extinction of morphine conditioned place preference with Tat-GluA2(3Y) interference peptide. Behav Brain Res. 2012 Aug 1;233(2):389-97. doi: 10.1016/j.bbr.2012.05.026. Epub 2012 May 23. PMID: 22633960.