PPTN

Name: PPTN
Brand: MedChemExpress
SKU: HY-110322A
Rating: 5.0 (4 reviews)

Cat. No.: HY-110322A Purity: 99.63%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a K_B value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity.

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

PPTN Chemical Structure

CAS No. : 1160271-30-6

Size	Stock	Quantity
1 mg	Get quote	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of PPTN:

PPTN hydrochloride Get quote

2 Publications Citing Use of MCE PPTN

: PPTN purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2022 Nov 30;114:109507. [Abstract]; HQL6 or PPTN significantly decreases the expressions of NLRP3, ASC and caspase-1 p20 in synovial tissue of rats.

: PPTN purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2022 Nov 30;114:109507. [Abstract]; HQL6 or PPTN significantly decreases the colocalization of NLRP3 and ASC in synovial tissues of rats. NLRP3 protein, ASC protein and nucleus are marked with Alexa Fluor 488 (Green), Alexa Fluor 647 (Red) and DAPI (Blue), respectively.

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View All Isoforms

P2Y1 Receptor P2Y2 Receptor P2Y6 Receptor P2Y12 Receptor P2Y13 Receptor P2Y14 Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

KB: 434 pM (P2Y14 receptor)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	14.5 nM Compound: 1	Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay	[PMID: 32787142]
CHO	IC₅₀	19 nM Compound: 1	Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay	[PMID: 32787142]
CHO	IC₅₀	6 nM Compound: 3; PPTN	Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R express Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R express	[PMID: 27331270]
CHO	IC₅₀	6 nM Compound: 1	Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed	[PMID: 32551012]
CHO	IC₅₀	9.75 nM Compound: 1	Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay	[PMID: 32787142]
HEK293	IC₅₀	21.6 nM Compound: 1	Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14	[PMID: 32551012]
HEK293	IC₅₀	21.6 nM Compound: 1	Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay	[PMID: 32787142]

In Vitro

PPTN exhibits strong selectivity for the P2Y14-R over the other seven nucleotide-activated P2Y receptors. 1 μM PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors^[1].
PPTN inhibits UDP-glucose-promoted chemotaxis in differentiated HL-60 human promyelocytic leukemia cells with IC₅₀s of ~1 nM in the presence of 10 μM UDP-glucose and ~4 nM in the presence of 100 μM^[1].
PPTN (10 µM) significantly decreases the ratios of p-ERK1/2 to ERK1/2 and p-p38 to p38^[2].

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

Molecular Weight

475.50

Formula

C₂₉H₂₄F₃NO₂

CAS No.

1160271-30-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC(C2=CC=C(C3CCNCC3)C=C2)=C4C=CC(C5=CC=C(C(F)(F)F)C=C5)=CC4=C1

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 : 22.22 mg/mL (46.73 mM; adjust pH to 7 with 1 M HCL; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1030 mL	10.5152 mL	21.0305 mL
5 mM	0.4206 mL	2.1030 mL	4.2061 mL
10 mM	0.2103 mL	1.0515 mL	2.1030 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.63%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (250 KB) HNMR (270 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Barrett MO, et al. A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils. Mol Pharmacol. 2013 Jul;84(1):41-9. [Content Brief]

[2]. Lin J, et al. The P2Y14 receptor in the trigeminal ganglion contributes to the maintenance of inflammatory pain. Neurochem Int. 2019 Dec;131:104567. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1030 mL	10.5152 mL	21.0305 mL	52.5762 mL
	5 mM	0.4206 mL	2.1030 mL	4.2061 mL	10.5152 mL
	10 mM	0.2103 mL	1.0515 mL	2.1030 mL	5.2576 mL
	15 mM	0.1402 mL	0.7010 mL	1.4020 mL	3.5051 mL
	20 mM	0.1052 mL	0.5258 mL	1.0515 mL	2.6288 mL
	25 mM	0.0841 mL	0.4206 mL	0.8412 mL	2.1030 mL
	30 mM	0.0701 mL	0.3505 mL	0.7010 mL	1.7525 mL
	40 mM	0.0526 mL	0.2629 mL	0.5258 mL	1.3144 mL

PPTN Related Classifications

Inflammation/Immunology

Help & FAQs

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.

Keywords:

PPTN1160271-30-6P2Y ReceptorP2Y14Anti-inflammatoryimmunep-ERK1/2ERK1/2p-p38p38Inhibitorinhibitorinhibit

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PPTN

Customer Review

Other Forms of PPTN:

PPTN Related Antibodies

2 Publications Citing Use of MCE PPTN

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Biological Activity

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References

Customer Review

PPTN Related Antibodies

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Complete Stock Solution Preparation Table

PPTN Related Classifications

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