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  3. Tat-NR2B9c

Tat-NR2B9c  (Synonyms: Tat-NR2Bct; NA-1)

Cat. No.: HY-P0117 Purity: 99.97%
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Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits?neuronal nitric oxide synthase (nNOS)/PSD-95?interaction, and possesses neuroprotective efficacy.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Tat-NR2B9c Chemical Structure

Tat-NR2B9c Chemical Structure

CAS No. : 500992-11-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
USD 731 In-stock
Solution
10 mM * 1 mL in Water USD 731 In-stock
Solid
1 mg USD 84 In-stock
5 mg USD 216 In-stock
10 mg USD 336 In-stock
25 mg USD 660 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Tat-NR2B9c:

Top Publications Citing Use of Products

    Tat-NR2B9c purchased from MedChemExpress. Usage Cited in: J Cereb Blood Flow Metab. 2019 Aug;39(8):1588-1601.  [Abstract]

    Tat-NR2B9c affects PSD95-NR2B-nNOS complex and PSD95-neurexin-neuroligin complex formation after ICH. Western blots of IP with PSD95 antibody show the interactions between nNOS, NR2B, neurexin-1 or neuroligin-1, and PSD95.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits?neuronal nitric oxide synthase (nNOS)/PSD-95?interaction, and possesses neuroprotective efficacy[1][2][5].

    IC50 & Target

    NMDA Receptor

     

    nNOS

     

    In Vitro

    Tat-NR2B9c is a PSD-95 inhibitor, with an EC50 of 6.7 nM for PSD-95d2, representing a >100-fold higher affinity for this domain than for PSD-95d1 (EC50, 0.67 μM). Tat-NR2B9c inhibits NMDAR2A, NMDAR2B, and NMDAR2C binding to PSD-95, with IC50s of 0.5 μM, ~8 μM, and 0.75 μM, respectively.
    Tat-NR2B9c also blocks the interaction between PSD-95 and nNOS with an IC50 of ~0.2 μM[1].
    Tat-NR2B9c reduces association of PSD-95 with GluN2B by ~50% in the YAC128 striatum, decreases NMDA-induced p38 activation in YAC128 striatal tissue, but shows no effect on the NMDA-induced JNK activation[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Tat-NR2B9c (10?nmol/g, i.v.) reduces infarction volume of male C57BL/6 mice, but has no effect at 3?nM/g[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    2518.88

    Formula

    C105H188N42O30

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    Sequence Shortening

    YGRKKRRQRRRKLSSIESDV

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Sealed storage, away from moisture

    Powder -80°C 2 years
    -20°C 1 year

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (39.70 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.3970 mL 1.9850 mL 3.9700 mL
    5 mM 0.0794 mL 0.3970 mL 0.7940 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

    • Protocol 1

      Tat-NR2B9c is prepared in saline[4].

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.97%

    References
    Cell Assay
    [2]

    Postnatal mono-cultured WT and YAC128 striatal neurons (DIV 9, due to the viability of these mono-cultured MSNs) are pretreated for 1 h with 200 nM Tat-NR2B9c, and/or SB-239063 (p38 inhibitor), and/or SP-600125 (JNK inhibitor), then incubated with or without 500 μM NMDA for 10 min. After NMDA treatment, striatal neurons are washed once with warm plating medium (PM) and then incubated in conditioned PM (without Tat peptides or p38, JNK inhibitors) for 24 h. Then cells are washed with PBS once and fixed with 4% paraformaldehyde (PFA) for 30 min[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mice[3]
    In each study mice are randomly allocated to three treatment groups (0.0, 3.0, 10.0 nMole/g Tat-NR2B9c) or to sham treatment. The individual performing the experimental procedures, administering treatments and performing the analyses is blinded to the treatment assignments. Tat-NR2B9c is prepared at the indicated doses and administered intravenously via the tail vein using a pump in a volume of 1 µL/g over 5 min beginning at reperfusion[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 0.3970 mL 1.9850 mL 3.9700 mL 9.9250 mL
    5 mM 0.0794 mL 0.3970 mL 0.7940 mL 1.9850 mL
    10 mM 0.0397 mL 0.1985 mL 0.3970 mL 0.9925 mL
    15 mM 0.0265 mL 0.1323 mL 0.2647 mL 0.6617 mL
    20 mM 0.0199 mL 0.0993 mL 0.1985 mL 0.4963 mL
    25 mM 0.0159 mL 0.0794 mL 0.1588 mL 0.3970 mL
    30 mM 0.0132 mL 0.0662 mL 0.1323 mL 0.3308 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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