2. GPCR/G Protein Apoptosis
  3. P2Y Receptor Necroptosis
  4. HDL-16

HDL-16 is a potent P2Y14R antagonist with an IC50 of 0.3095 nM. HDL-16 ameliorates DSS (HY-116282C)-induced colitis through suppressing necroptosis of intestinal epithelium cells (IECs) and protecting mucosal barrier function.

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HDL-16 Chemical Structure

HDL-16 Chemical Structure

CAS No. : 2373280-36-3

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HDL-16 Related Antibodies

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Description

HDL-16 is a potent P2Y14R antagonist with an IC50 of 0.3095 nM. HDL-16 ameliorates DSS (HY-116282C)-induced colitis through suppressing necroptosis of intestinal epithelium cells (IECs) and protecting mucosal barrier function[1].

IC50 & Target[1]

P2Y14 Receptor

0.3095 nM (IC50)

In Vitro

The N atom on benzoxazole ring of HDL-16 forms a hydrogen bond with Tyr102 residue, and the amine group also forms a hydrogen bond interaction with His184 residue in the binding pocket of P2Y14R[1].
HDL-16 has almost no cytotoxicity under the concentration of 10 μM in HT-29 cells[1].
HDL-16 can inhibit the necroptosis of HT-29 cells (with 20 ng/mL TNF‐α plus 20 μM z‐VAD‐fmk (HY-16658B) and Smac mimetic (BV6, 2 μM) for 8 h)[1].

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

HDL-16 Related Antibodies
In Vivo

HDL-16 (10 μM or 20 μM; 100 μL; Rectally administered; daily; 6 days) with high-dose significantly suppresses colitis symptoms and leads to maintained gut barrier integrity in the mice[1].

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

Animal Model: Male, 7-8-week-old, P2Y14Rfl/fl Vil-cre (P2Y14R∆IEC), P2Y14Rfl/fl Lyz2-cre and WT mice with C57BL/6 J background[1]
Dosage: 10 μM or 20 μM; 100 μL
Administration: Rectally administered; daily; 6 days
Result: With high-dose showed dramatically less body weight loss and lower Disease Activity Index (DAI) than Dextran sodium sulfate (DSS; 36-50 kDa; 3% w/v; drinking water for 7 days)-exposed mice.
With high-dose improved DSS-induced inflammatory infiltration and tissue damage.
With high-dose resulted in a prominently suppression in necroptosis of the IECs in DSS-treated mice.
Molecular Weight

303.15

Formula

C14H11BrN2O
CAS No.
SMILES

BrC(C=C1)=CC=C1NCC2=NC3=CC=CC=C3O2
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Room temperature in continental US; may vary elsewhere.
Storage

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

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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

    0.1% DMSO + 99.9% Saline

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Purity & Documentation
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HDL-16 Related Classifications

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:

HDL-162373280-36-3HDL16HDL 16P2Y ReceptorNecroptosisP2Y14RDSSintestinal epithelium cellsIECsmucosal barrierTyr102colitisInhibitorinhibitorinhibit

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