Cat. No.: HY-108960

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PPADS

Name: PPADS
Brand: MedChemExpress
SKU: HY-108960
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10 Cited Publications

고객리뷰

Based on 10 publication(s) in Google Scholar

PPADS is a P2X receptor (P2X Receptor) antagonist and a reversible competitive antagonist of NAADP receptors, with IC₅₀ values of 68 nM (P2X1) and 214 nM (P2X3), respectively. PPADS alleviates pain-related behaviors in the central and peripheral nervous systems of mice after peripheral neuropathy, inhibits the overproduction of IL-1β, IL-6, iNOS and nNOS, and suppresses the hydrolytic activity of extracellular ATPase. PPADS blocks ATP-mediated inward currents on recombinant rat P2X₁ and P2X₃ receptors, and inhibits purinergic nerve stimulation-induced contraction of rabbit bladder detrusor muscle. PPADS is applicable to research related to neuropathic pain.

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CAS No.: 149017-66-3
화학식: C₁₄H₁₄N₃O₁₂PS₂
분자량:511.38

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (281 KB)

PPADS Chemical Structure

CAS No.: 149017-66-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

p2x1 Receptor

68 nM (IC₅₀)

P2X2 Receptor

214 nM (IC₅₀)

All P2X Receptor Isoforms :

All Interleukin Related Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Oocyte	IC₅₀	0.099 μM Compound: 1	Inhibition of inward ion current elicited by ATP at P2X1 receptor expressed in Xenopus oocytes Inhibition of inward ion current elicited by ATP at P2X1 receptor expressed in Xenopus oocytes	[PMID: 11462975]
Oocyte	IC₅₀	0.24 μM Compound: 1	Inhibition of inward ion current elicited by ATP was determined at recombinant P2X3 receptor expressed in Xenopus oocytes Inhibition of inward ion current elicited by ATP was determined at recombinant P2X3 receptor expressed in Xenopus oocytes	[PMID: 11462975]
Oocyte	IC₅₀	1.6 μM Compound: 1	Inhibition of inward ion current elicited by ATP at P2X2 receptor expressed in Xenopus oocytes Inhibition of inward ion current elicited by ATP at P2X2 receptor expressed in Xenopus oocytes	[PMID: 11462975]
Oocyte	EC₅₀	240 nM Compound: PPADS	The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 3 (P2X3) at 10 uM, expressed in Xenopus oocytes The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 3 (P2X3) at 10 uM, expressed in Xenopus oocytes	[PMID: 12213051]
Oocyte	EC₅₀	99 nM Compound: PPADS	The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 1 (P2X1) at 1 uM, expressed in Xenopus oocytes The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 1 (P2X1) at 1 uM, expressed in Xenopus oocytes	[PMID: 12213051]
Oocyte	EC₅₀	>10000 nM Compound: PPADS	Antagonist activity against recombinant rat P2X purinoceptor 4 (P2X4) at 3 uM, expressed in Xenopus oocytes Antagonist activity against recombinant rat P2X purinoceptor 4 (P2X4) at 3 uM, expressed in Xenopus oocytes	[PMID: 12213051]
Oocyte	EC₅₀	12 μM Compound: PPADS	The compound was evaluated for antagonist activity against recombinant rat receptor P2X purinoceptor 2 (P2X2) at 30 uM, expressed in Xenopus oocytes The compound was evaluated for antagonist activity against recombinant rat receptor P2X purinoceptor 2 (P2X2) at 30 uM, expressed in Xenopus oocytes	[PMID: 12213051]
Oocyte	IC₅₀	240 μM Compound: 1b	Compound was tested in a functional ion channel assay of ATP-induced current at recombinant rat P2X3 receptor expressed in Xenopus oocytes. Compound was tested in a functional ion channel assay of ATP-induced current at recombinant rat P2X3 receptor expressed in Xenopus oocytes.	[PMID: 9632352]
Oocyte	IC₅₀	98.5 μM Compound: 1b	Compound was tested in a functional ion channel assay of ATP-induced current at recombinant rat P2X1 receptor expressed in Xenopus oocytes. Compound was tested in a functional ion channel assay of ATP-induced current at recombinant rat P2X1 receptor expressed in Xenopus oocytes.	[PMID: 9632352]

In Vitro

PPADS (1-100 μM; 1 min) acts as a competitive, partially surmountable antagonist of NAADP (HY-103317)-induced Ca²⁺ release in sea urchin egg homogenate, with an IC₅₀ of 20.6 μM^[2].
PPADS (100 μM) inhibits the transport of NAADP into NIH-3T3 cells, with an inhibition rate of 31.1%^[2].
PPADS (0.01-30,000 nM; 20 min) potently inhibits ATP (HY-B2176)-evoked inward currents at rat P2X₁ and P2X3 receptors expressed in Xenopus laevis oocytes via non-competitive antagonism (partially reversible after washing), with IC₅₀ values of 68.5 nM and 213.6 nM, respectively^[3].
PPADS (1-30 μM; for at least 20 min) concentration-dependently antagonizes the α,β-methylene ATP-induced contraction of rabbit urinary bladder detrusor muscle mediated by P₂_x-purinergic receptors^[4].
PPADS (1-30 μM; at least 20 min) concentration-dependently antagonizes purinergic neurogenic contractions of rabbit detrusor muscle^[4].

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

In Vivo

PPADS (6.25-25 mg/kg, i.p.; once daily; 11 days (chronic); single administration (acute, on day 3 or day 14 post-injury)) dose-dependently reverses neuropathic pain behaviors in CCI mice. The 25 mg/kg dose fully restores physiological nociceptive thresholds, and simultaneously normalizes the abnormal expressions of proinflammatory cytokines, nitric oxide synthase, NF-κB and myelin proteins in peripheral and central pain signaling pathways^[1].

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

Animal Model:

C57BL/6J (male, 20-25 g, chronic constriction injury of sciatic nerve)^[1]
Dosage:

6.25-25 mg/kg (chronic administration); 25 mg/kg (acute administration)
Administration:

i.p.; once daily, 11 days (chronic); single dose (acute, day 3 or 14 post-injury)
Result:

Dose-dependently reduced thermal hyperalgesia and mechanical allodynia.
Completely abolished both hypersensitivity and restored physiological thresholds at 25 mg/kg (chronic).
Reduced overexpression of IL-1β mRNA and protein in ipsilateral sciatic nerve, L4-L6 dorsal root ganglia, and L4-L6 spinal cord dorsal horn at 25 mg/kg (chronic).
Reduced IL-6 mRNA overexpression in ipsilateral sciatic nerve (day 14 post-injury only) at 25 mg/kg (chronic).
Normalized increased nNOS and iNOS protein levels in ipsilateral sciatic nerve, L4-L6 dorsal root ganglia, and L4-L6 spinal cord dorsal horn at 25 mg/kg (chronic).
Abolished doubled nNOS protein level in contralateral thalamus relative to ipsilateral thalamus at 25 mg/kg (chronic).
Reversed NF-κB activation in ipsilateral sciatic nerve at 25 mg/kg (chronic).
Restored reduced P0 myelin protein mRNA levels in ipsilateral sciatic nerve to physiological levels at 25 mg/kg (chronic).
Reversed mechanical allodynia at 1 hour post-administration (effect absent by 24 hours) without modifying thermal hyperalgesia when given at day 3 post-injury (acute 25 mg/kg).
Produced identical effects on mechanical allodynia and thermal hyperalgesia as day 3 acute dose when given at day 14 post-injury (acute 25 mg/kg).

Chemical Information

CAS No. 149017-66-3
분자량 511.38
화학식 C₁₄H₁₄N₃O₁₂PS₂
SMILES

O=CC1=C(C(C)=NC(/N=N/C2=CC=C(S(=O)(O)=O)C=C2S(=O)(O)=O)=C1COP(O)(O)=O)O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (10)

All OthersIn Vivo Efficacy Study

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Mil Med Res

PANX1-mediated ATP release confers FAM3A's suppression effects on hepatic gluconeogenesis and lipogenesis. [Abstract]

2024 Jun 27;11(1):41. PMID: 38937853

PPADS purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2024 Jun 27;11(1):41. [Abstract]

The effect of PANX1 inhibitor PBN, pan P2 receptor inhibitor suramin, pan P2X inhibitor PPADS (50 μM),specific P2Y1 inhibitor MRS2179 or specific P2Y12 inhibitor PSB-0739 on the glucose production in mouse hepatocytes.
Mol Psychiatry

ATP release from the amygdala-prefrontal pathway regulates vulnerability to social stress in male mice. [Abstract]

2026 Mar 27. PMID: 41896365
J Med Chem

A Novel Compound 3a-M1, from Metabolites of Sinomenine Derivative 3a, Exerts Potent Anti-Aplastic Anemia Activity via IP3R/ORAI-Mediated CTL Ferroptosis. [Abstract]

2025 Apr 17. PMID: 40243551
Int Immunopharmacol

The immunoregulator β-glucan produces antidepressant effects through microglia-mobilized astrocytic P2Y1R-BDNF signaling in the dentate gyrus. [Abstract]

2025 Sep 6:165:115494. PMID: 40915186
ACS Chem Neurosci

Optical Precise Ablation of Targeted Individual Neurons In Vivo. [Abstract]

2025 Feb 5;16(3):374-383. PMID: 39800970
J Biol Chem

Type 2 diabetic mice enter a state of spontaneous hibernation-like suspended animation following accumulation of uric acid. [Abstract]

2021 Oct;297(4):101166. PMID: 34487763

PPADS purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2021 Oct;297(4):101166. [Abstract]

The time of each stage of the hibernation-like state induced by ATP after using receptor antagonist of P2X (suramin, 75 mmol/kg, i.p., 1 h before ATP-injection) or P2Y (PPADS, 140 mmol/kg, i.p., 1 h before ATP-injection).
J Endocrinol Invest

Pannexin-1 regulation of ATP release promotes the invasion of pituitary adenoma. [Abstract]

2025 Feb;48(2):317-332. PMID: 39527372
Pharmacol Biochem Behav

Intranasal LAG3 antibody infusion induces microglia-dependent antidepressant effect by mobilizing astrocytic P2Y1R-mediated BDNF synthesis in the hippocampus. [Abstract]

2025 Dec:257:174114. PMID: 41106438

PPADS purchased from MedChemExpress. Usage Cited in: Pharmacol Biochem Behav. 2025 Dec:257:174114. [Abstract]

Quantitative analysis shows that antagonism of P2X1R, P2X2R, P2X3R, P2X5R and P2X7R in the hippocampus by PPADS (20 μg) had no effect on In-LAG3-Ab-induced decrease in immobility time in the TST.
bioRxiv

2024 November 03.
bioRxiv

2023 Sep 17.

순도&문서

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Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Martucci C, et al. The purinergic antagonist PPADS reduces pain related behaviours and interleukin-1 beta, interleukin-6, iNOS and nNOS overproduction in central and peripheral nervous system after peripheral neuropathy in mice. Pain. 2008;137(1):81-95. [Content Brief]

[2]. Billington RA, et al. PPADS is a reversible competitive antagonist of the NAADP receptor. Cell Calcium. 2007;41(6):505-511. [Content Brief]

[3]. Brown SG, et al. Actions of a Series of PPADS Analogs at P2X1 and P2X3 Receptors. Drug Dev Res. 2001 Aug;53(4):281-291. [Content Brief]

[4]. Ziganshin AU, et al. PPADS selectively antagonizes P2X-purinoceptor-mediated responses in the rabbit urinary bladder. Br J Pharmacol. 1993;110(4):1491-1495. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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PPADS

A 438079 hydrochloride

2-Methylthio-AMP

NF110

A 438079

5-BDBD

Camlipixant

α,β-Methylene-ATP trisodium

NF449 octasodium

A 438079 hydrochloride (Standard)

A-740003

Brilliant blue G-250

Gefapixant

Publications Citing Use of MedChemExpress (MCE) PPADS

All P2X Receptor Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Publications (10)

순도&문서

References

Calculators

Help & FAQs

Bioz

PPADS

A 438079 hydrochloride

2-Methylthio-AMP

NF110

A 438079

5-BDBD

Camlipixant

α,β-Methylene-ATP trisodium

NF449 octasodium

A 438079 hydrochloride (Standard)

A-740003

Brilliant blue G-250

Gefapixant

Publications Citing Use of MedChemExpress (MCE) PPADS

All P2X Receptor Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Publications (10)

순도&문서

References

Calculators

Help & FAQs

PPADS Related Classifications

HY-108960 Related Classifications

Bioz