1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. JNJ-47965567

JNJ-47965567 

Cat. No.: HY-101418 Purity: 98.63%
Handling Instructions

JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.

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

JNJ-47965567 Chemical Structure

JNJ-47965567 Chemical Structure

CAS No. : 1428327-31-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 108 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 195 In-stock
Estimated Time of Arrival: December 31
25 mg USD 395 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology[1].

IC50 & Target

pKi: 7.9 (huaman P2X7), 8.7 (rat P2X7)[1]

In Vitro

JNJ-47965567 exhibits high affinity for human and rat P2X7 in membrane preparations of 1321N1 cells[1].
JNJ-47965567 does not block IL-6 and TNF-α release, under identical conditions (LPS and BZ-ATP) used for IL-1β and IL-18 release[1].
JNJ-47965567 attenuates IL-1β release with pIC50s of 6.7 ± 0.07 (human blood), 7.5 ± 0.07 (human monocytes) and 7.1 ± 0.1 (rat microglia), respectively, in native systems[1].

In Vivo

JNJ-47965567 (30-100 mg/kg; s.c.) attenuates IL-1β release induced by Bz-ATP[1].
JNJ-47965567 (30 mg/kg) attenuates amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain[1].

Animal Model: Male Sprague Dawley rats[1]
Dosage: 30 mg/kg, 100 mg/kg
Administration: Subcutaneous injection; 30 minutes prior to Bz-ATP infusion
Result: Significantly attenuated IL-1β release at 100 mg/kg, with no effect at 30 mg/kg dose group.
Molecular Weight

488.64

Formula

C₂₈H₃₂N₄O₂S

CAS No.

1428327-31-4

SMILES

O=C(C1=CC=CN=C1SC2=CC=CC=C2)NCC3(N4CCN(C5=CC=CC=C5)CC4)CCOCC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (51.16 mM; ultrasonic and warming and heat to 50°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0465 mL 10.2325 mL 20.4650 mL
5 mM 0.4093 mL 2.0465 mL 4.0930 mL
10 mM 0.2046 mL 1.0232 mL 2.0465 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

JNJ-47965567JNJ47965567JNJ 47965567P2X ReceptorP2XRsP2X7neuropathicpainInhibitorinhibitorinhibit

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JNJ-47965567
Cat. No.:
HY-101418
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