1. GPCR/G Protein
  2. P2Y Receptor
  3. 2-MeSADP

2-MeSADP  (Synonyms: 2-Methylthioadenosine diphosphate; 2-Methylthio-ADP)

Cat. No.: HY-108648A
Handling Instructions Technical Support

2-MeSADP is a P2Y receptor agonist, with an EC50 of 5 nM for human P2Y12, EC50 values of 19 nM and 13 nM for human P2Y13, and an EC50 of 6.2 nM for mouse P2Y13. It shows slightly higher selectivity for P2Y12 over human P2Y13. 2-MeSADP triggers increases in intracellular calcium levels, Gi-mediated cAMP inhibition, adenylate cyclase inhibition and downstream signal transduction. 2-MeSADP can be used in research related to glaucoma.

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

2-MeSADP

2-MeSADP Chemical Structure

CAS No. : 34983-48-7

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Description

2-MeSADP is a P2Y receptor agonist, with an EC50 of 5 nM for human P2Y12, EC50 values of 19 nM and 13 nM for human P2Y13, and an EC50 of 6.2 nM for mouse P2Y13. It shows slightly higher selectivity for P2Y12 over human P2Y13. 2-MeSADP triggers increases in intracellular calcium levels, Gi-mediated cAMP inhibition, adenylate cyclase inhibition and downstream signal transduction. 2-MeSADP can be used in research related to glaucoma[1][2][3][4].

IC50 & Target

P2Y13 Receptor

19 nM (EC50)

P2Y12 Receptor

5 nM (EC50)

Cellular Effect
Cell Line Type Value Description References
COS-7 EC50
1.27 nM
Compound: 2-MeSADP
Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
1.58 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human S317A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human S317A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
100 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human H277A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human H277A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
11.2 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human T222A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human T222A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
11.7 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human S314T mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human S314T mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
12.6 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human Y136A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human Y136A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
145 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human D204E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human D204E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
14800 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R287A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R287A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
15 nM
Compound: 2-MeSADP
Effective concentration to activate human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration to activate human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
15.9 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human H132A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human H132A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
15.9 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human T221A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human T221A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
16 nM
Compound: 2-MeSADP
Effective concentration to activate human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration to activate human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
17.5 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human K198A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human K198A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
17200 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human E209A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human E209A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
1790 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human K280A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human K280A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
18.2 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human F131A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human F131A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
19 nM
Compound: 2-MeSADP
Effective concentration to activate human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration to activate human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
2.2 nM
Compound: 2-MeSADP
Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate is determined in separate experiment
Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate is determined in separate experiment
[PMID: 15481977]
COS-7 EC50
2.5 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human K196A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human K196A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
2.6 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R301A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R301A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
20.7 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human F226A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human F226A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
3 nM
Compound: 2-MeSADP
Effective concentration to activate wild-type P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration to activate wild-type P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
3.2 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human E209D mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human E209D mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
3.6 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human D208A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human D208A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
3.9 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human D289A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human D289A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
4.7 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R195A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R195A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
4.9 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human E209R mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human E209R mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
418 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R310K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R310K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
455 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human Q307A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human Q307A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
5.9 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human K125A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human K125A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
5160 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human C296A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human C296A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
5290 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R287Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R287Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
595 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human D204N mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human D204N mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
6 nM
Compound: 2-MeSADP
Effective concentration to activate human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration to activate human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
66.5 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human D204A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human D204A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
7.8 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R212A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R212A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
74.9 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R287K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R287K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
8.6 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human E209Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human E209Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
9.2 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R285A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R285A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
9.8 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human D300A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human D300A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
> 10000 nM
Compound: 2-MeSADP
Effective concentration to activate human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration to activate human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
> 10000 nM
Compound: 2-MeSADP
Effective concentration to activate human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration to activate human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
> 100000 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human C124A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human C124A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
> 100000 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human C202A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human C202A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
> 100000 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R128A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R128A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
> 100000 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R287E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R287E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
> 100000 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human R310A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human R310A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 EC50
> 100000 nM
Compound: 2-MeSADP
Effective concentration required for the activation of human S314A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
Effective concentration required for the activation of human S314A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
[PMID: 15481977]
COS-7 IC50
150 nM
Compound: 2-MeSADP
Inhibition concentration required against human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
Inhibition concentration required against human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
[PMID: 15481977]
COS-7 IC50
22 nM
Compound: 2-MeSADP
Inhibition concentration required against human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand
Inhibition concentration required against human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand
[PMID: 15481977]
COS-7 IC50
24 nM
Compound: 2-MeSADP
Inhibition concentration required against wild type strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand
Inhibition concentration required against wild type strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand
[PMID: 15481977]
COS-7 IC50
260 nM
Compound: 2-MeSADP
Inhibition concentration required against human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
Inhibition concentration required against human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
[PMID: 15481977]
COS-7 IC50
360 nM
Compound: 2-MeSADP
Inhibition concentration required against human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
Inhibition concentration required against human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
[PMID: 15481977]
COS-7 IC50
40 nM
Compound: 2-MeSADP
Inhibition concentration required against human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
Inhibition concentration required against human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
[PMID: 15481977]
COS-7 IC50
> 10000 nM
Compound: 2-MeSADP
Inhibition concentration required against human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
Inhibition concentration required against human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand
[PMID: 15481977]
HEK293 EC50
0.1 μM
Compound: 2-MeS-ADP
Activity against rat P2Y1-GFP transfected in HEK293 cells by intracellular calcium increase
Activity against rat P2Y1-GFP transfected in HEK293 cells by intracellular calcium increase
[PMID: 16539385]
In Vitro

2-MeSADP (Serial dilutions) potently activates human SP174 (P2Y13) in HEK293-EBNA cells cotransfected with Gαq/i3, with an EC50 of 19 nM, making it one of the most potent ligands tested for this receptor[1].
2-MeSADP (Serial dilutions) potently activates mouse SP174 (P2Y13) in HEK293-EBNA cells cotransfected with Gαq/i3, with an EC50 of 6.2 nM, showing higher potency at the murine receptor than the human ortholog[1].
2-MeSADP (Serial dilutions; 10 min) potently inhibits forskolin-stimulated cAMP accumulation in HEK293-EBNA cells stably transfected with human SP174 (P2Y13), with an EC50 of 13 nM, confirming coupling of the receptor to Gαi signaling[1].
2-MeS-ADP (Serial dilutions) potently activates human P2Y12 in HEK293-EBNA cells cotransfected with Gαq/i3, with an EC50 of 5 nM, showing higher potency at P2Y12 than at the related SP174 (P2Y13) receptor[1].
2-MeSADP (0.2 mg; 3 h) is partially susceptible to hydrolysis by alkaline phosphatase, with 87% degradation observed after a 3-hour incubation at 37 °C[2].
2-MeSADP (40 mM; up to 24 h) exhibits moderate metabolic stability in human blood serum, with a half-life of 23.5 h at 37 °C[2].
2-MeSADP (multiple concentrations) potently activates the turkey P2Y1 receptor expressed in human 1321N1 astrocytoma cells, inducing intracellular Ca 2+ mobilization with an EC50 of 0.0025 μM[2].
2-MeSADP (log M values of -7 to -5.5) induces aggregation and shape change in human platelets, and is 3-5 times more potent as an aggregating agent than ADP[4].
2-MeSADP (log M values of -9 to -7; 2 min) potently inhibits PGE1-stimulated cyclic AMP accumulation in human platelets, with half-maximal inhibition at 6 nM in platelet-rich plasma and 2 nM in washed platelets, and is 150-200 times more potent than ADP for this effect[4].

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

Molecular Weight

473.29

Formula

C11H17N5O10P2S

CAS No.
SMILES

O[C@H]1[C@@H](O)[C@H](N2C=NC3=C2N=C(SC)N=C3N)O[C@@H]1COP(OP(O)(O)=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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2-MeSADP
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