Cat. No.: HY-P12399

SP16 peptide

SP16 peptide is a LRP1 signaling-activating peptide and anti-inflammatory agent that crosses the blood-brain barrier. SP16 peptide activates the Akt/ERK pro-survival signaling pathway, downregulates TLR4, and inhibits NF-κB, inflammasome formation, ROS production, pro-apoptotic signaling, caspase activity, and inflammatory cytokine release. SP16 peptide exhibits cardioprotective, neuroprotective, and analgesic effects, attenuating myocardial injury and preserving left ventricular function while alleviating allodynia and nociceptive behavior. SP16 peptide restores HIV-impaired barrier integrity and reduces HIV replication and cytokine and chemokine secretion. SP16 peptide can be used in research related to acute myocardial infarction, acute pain, inflammatory and neuropathic pain, HIV infection, and non-alcoholic fatty liver disease.

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

CAS No.: 2640117-95-7
Formula: C₁₀₂H₁₆₀N₂₄O₂₄
Molecular Weight:2106.51

Storage:

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

SP16 peptide Chemical Structure

CAS No.: 2640117-95-7

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Akt Isoforms :

All ERK Isoforms :

All Toll-like Receptor (TLR) Isoforms :

All NF-κB Isoforms :

All Caspase Isoforms :

All NOD-like Receptor (NLR) Isoforms :

All Interleukin Related Isoforms :

All HIV Isoforms :

In Vitro

Cardiovascular RegulationInnate ImmunityCytokines & ChemokinesInflammasomeViral InfectionLocal Vascular RegulationOthers

Cardiovascular Regulation

SP16 (100 µg/mL; 1 h) inhibits NF-κB p65 nuclear translocation in human brain microvascular endothelial cells, and this effect is reversed by LRP1 siRNA knockdown^[3].

Innate Immunity

SP16 peptide (100 μg/mL; pre-incubation for 30 min) inhibits LPS (HY-D1056)- and Gp96-induced NF-κB activation in THP1-XBlue-MD2-CD14 monocytes, and this effect is attenuated by LRP1 blockade^[1].
SP16 (25-100 µg/mL; 12 h) reduces MCP-1, RANTES, and IL-6 secretion in primary human astrocytes, and this effect is reversed by an anti-LRP1 blocking antibody, confirming LRP1 dependence^[3].

Innate Immunity

Cytokines & Chemokines

Inflammasome

SP16 peptide (100 μg/mL; 4 h) inhibits NLRP3 inflammasome activation in J774A.1 macrophages^[1].

Viral Infection

Cytokines & Chemokines

SP16 peptide (1-100 µg/mL; 12 h) reduces MCP-1 and attenuates p24^[3] in HIV-1 SF162-infected HMC3 microglia without BBB inserts.
SP16 peptide (1-150 µg/mL; 6-12 h) reduces p24 and decreases HIV-induced MCP-1 in HIV-1 SF162-infected primary human astrocytes^[3].
SP16 peptide (25-250 µg/mL; 12 h) reduces MCP-1, IL-8, and p24 in HIV-1 SF162-infected primary human BMECs^[3].

Viral Infection

Cytokines & Chemokines

Innate Immunity

SP16 peptide (25-250 µg/mL; 12 h) reduces MCP-1, IL-6, and p24 in EcoHIV-infected mouse mixed glial cells^[3].

Viral Infection

Innate Immunity

SP16 peptide (25 µg/mL; 12 h) upregulates Akt without changing NF-κB in primary human astrocytes and endothelial cells, but higher concentrations decrease NF-κB^[3].

Viral Infection

Local Vascular Regulation

SP16 peptide (25-150 µg/mL; 6 h) crosses the artificial human BBB and restores HIV-impaired FITC-dextran permeability without disrupting TEER^[3].

Others

SP16 peptide (1-5 μg/mL; 1 h) binds recombinant human LRP1^[1] in vitro in a streptavidin pull-down assay.
SP16 (0-500 ng/mL) promotes neurite outgrowth and neuronal survival in primary adult rat DRG neurons^[2].
SP16 increases GAP-43 mRNA in primary adult rat DRG cultures^[2].
SP16 (2.4-240 nM; 5-30 min) activates Akt and ERK1/2 in rat PC12 cells, but GST-RAP blocks this activation^[2].
SP16 (48 h) activation of ERK1/2 in rat PC12 cells requires LRP1, and siLRP1 reduces LRP1 mRNA by 70%^[2].
SP16 peptide (25-250 µg/mL; 24-96 h) does not reduce the viability of HMC3 microglia or primary human astrocytes and BMECs^[3].

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

ELISA Assay^[1]

Cell Line:

J774A.1 macrophages
Concentration:

100 μg/mL
Incubation Time:

4 h (LPS or Gp96); 2 h (Nigericin (HY-127019) or ATP (HY-B2176))
Result:

Inhibited mature IL-1β levels by >50% following stimulation with LPS and Nigericin or Gp96 and ATP.

Western Blot Analysis^[2]

Cell Line:

rat PC12 cells
Concentration:

2.4, 24, 240 nM
Incubation Time:

5, 10 and 30 min
Result:

Activated phospho-ERK1/2 at concentrations as low as 24 nM.
Robustly activated ERK1/2 from 5-30 min.
Activated Akt and ERK1/2 in PC12 cells, and addition of GST-RAP blocked activation of both Akt and ERK1/2.

ELISA Assay^[3]

Cell Line:

HMC3 microglia infected or not infected with HIV-1 SF162, cultured with and without BBB inserts
Concentration:

1 and 100 µg/mL
Incubation Time:

12 h
Result:

MCP-1 secretion decreased by more than 50% in both non-infected and HIV-infected microglia with and without BBB inserts; the decrease was concentration-dependent.
IL-6 and IL-8 secretion decreased in supernatant from microglia without the BBB insert.
p24 was attenuated in a concentration-dependent manner in microglia without the BBB insert.
In cells with BBB inserts, IL-6, IL-8, and p24 were unaffected.

Parmacokinetics

Species	Dose	Route	C_max	Clearance (CL)	MRT	T_1/2β	V_dss
Rat^[1]	5 mg/mL	i.v.	1.5 mg/mL	/	/	/	/
Rat^[1]	25 mg/kg	i.v.	16.4 mg/mL	216 mL/min/kg	15 min	3.3 h	3.4 L/kg

In Vivo

Anti-cancerAdaptive ImmunityInnate ImmunityCytokines & ChemokinesImmune Tolerance & ImmunosuppressionLipid MetabolismBacterial InfectionCardiovascular RegulationRegulation of Cardiac Pump FunctionApoptosisViral InfectionOthers

Anti-cancer

Adaptive Immunity

Innate Immunity

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

Lipid Metabolism

SP16 peptide (100-120 µg/mouse; intraperitoneal and subcutaneous injection; 2-3 times per week; 5-7 weeks or until sacrifice) restores CD4⁺ T cells but does not modulate the hepatic immunological pattern and does not prevent NAFLD-related HCC^[4].

Bacterial Infection

SP16 peptide (12 µg total; intraperitoneal injection; 4 µg administered at -2 h, 0 h, and 0.5 h before LPS (HY-D1056) challenge) improves the survival rate of mice with lethal endotoxemia^[1].

Cardiovascular Regulation

Regulation of Cardiac Pump Function

Apoptosis

SP16 peptide (10-100 µg; intraperitoneal injection; single dose) reduces myocardial infarct size and protects left ventricular systolic function after ischemia-reperfusion in mice^[1].

Cytokines & Chemokines

Lipid Metabolism

SP16 peptide (60 µg/mouse; intraperitoneal injection; three times per week; 12 weeks) modulates serum inflammatory cytokines/chemokines in diet-induced NAFLD^[4].

Innate Immunity

SP16 peptide (2 μg/g; subcutaneous injection; daily; injected 1 hr before PNL and continued for 2 weeks) prevents tactile allodynia after partial nerve ligation and inhibits inflammatory cell recruitment and satellite cell activation^[2].

Regulation of Cardiac Pump Function

SP16 peptide (3-500 µg; subcutaneous injection; single dose) reduces infarct size in experimental acute myocardial infarction^[1].

Viral Infection

Cytokines & Chemokines

Innate Immunity

SP16 peptide (10 µg/kg; intranasal administration; once every other day; until day 5 after cART initiation) combined with cART reduces MCP-1, RANTES, p24 gag, and NF-κB in the brain of EcoHIV-NDK-infected male C57BL/6J mice, while increasing Akt^[3].

Others

SP16 peptide (0.02-2 μg/g; subcutaneous injection; single injection 1 hr before intraplantar formalin injection) attenuates formalin-induced early and late nociceptive behaviors^[2].
SP16 peptide (2 μg/g; subcutaneous injection; single injection 1 hr before capsaicin injection) attenuates capsaicin-induced acute nociceptive behavior in male and female mice^[2].

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

Animal Model:

BALB/c (female)^[1]
Dosage:

doses of 4
μg, total of 12 μg
Administration:

i.p.; at -2 h, 0 h, and 0.5 h before LPS challenge; monitored for 72 h
Result:

Mortality at 72 h decreased from 100% to 40%.

Animal Model:

CD1 (outbred, male, 10 weeks of age)^[1]
Dosage:

10 µg; 100 µg
Administration:

i.p.; immediately after reperfusion
Result:

Infarct size was 7% of left ventricle, and cardiac troponin I at 24 h was 1.0 ng/mL.
Myocardial pAkt/total Akt ratio increased and Bax/Bcl2 ratio and caspase-3 activity decreased after 30 min ischemia and 180 min reperfusion.
At 7 days, left ventricular fractional shortening was greater and wall-motion abnormality was smaller; hearts showed reduced fibrotic scar, reduced cardiomyocyte apoptosis in the peri-infarct border zone, and reduced leukocyte infiltration.
The infarct-sparing effect was eliminated by LRP1 blocking antibody.

Animal Model:

CD1 (outbred, male, 10 weeks of age)^[1]
Dosage:

3 µg; 10 µg; 100 µg; 500 µg
Administration:

s.c.; after reperfusion; single dose
Result:

Subcutaneous administration after reperfusion produced a similar reduction in infarct size to corresponding intraperitoneal doses.

Animal Model:

C57BL/6J (male, 8-12 weeks old, 25 g)^[2]
Dosage:

0.02 μg/g; 0.2 μg/g; 2 μg/g
Administration:

s.c.; single administration 1 hr before intraplantar formalin
Result:

Early-phase licking time was 80 s at 0.02 μg/g and 60 s at 2 μg/g.
In the late phase, 0.2 μg/g and 2 μg/g reduced licking time; 2 μg/g delayed the late-phase peak start to 30 min.

Animal Model:

C57BL/6J (male and female, 8-12 weeks old, 25 g)^[2]
Dosage:

2 μg/g
Administration:

s.c.; single administration 1 hr before capsaicin
Result:

Blocked capsaicin-induced acute pain-related behavior in male mice and produced similar effects in female mice.

Animal Model:

C57BL/6J (male, 8-12 weeks old, 25 g)^[2]
Dosage:

2 μg/g (100 μL)
Administration:

s.c.; daily; 1 hr before PNL and then for 2 weeks
Result:

Prevented development of tactile allodynia; the anti-allodynic effect was most pronounced on days 2 and 4 and sustained through day 9.
In injured sciatic nerve, reduced CD11b levels by 10-fold and completely blocked injury-induced TLR4 upregulation.
In injured L4 DRGs, mice had approximately 5-fold less CD11b immunoreactivity and a 6-fold decrease in GFAP levels.

Animal Model:

C57BL/6J (male, 4-6 months old)^[3]
Dosage:

10 µg/kg
Administration:

intranasal; every other day; until day 5 after cART initiation
Result:

In EcoHIV-infected mouse brains, MCP-1 was reduced by 48% versus cART alone and RANTES was reduced by 35% versus cART alone.
p24 gag was further reduced by 19% relative to cART alone.
NF-κB protein was reduced by about 86% versus cART alone and Akt protein was increased by about 18% versus cART alone.
LRP-1 expression increased.

Animal Model:

DIAMOND (male; 2 months old at diet initiation)^[4]
Dosage:

60 µg/mouse
Administration:

i.p.; three times per week; 12 weeks
Result:

Serum inflammatory cytokines/chemokines were modulated after initiation at 16 weeks of WD.

Animal Model:

DIAMOND (male; 2 months old at diet initiation)^[4]
Dosage:

100 µg/mouse; 120 µg/mouse
Administration:

i.p.; 120 μg/mouse; three times per week; 5 weeks; i.p.; 100 μg/mouse; three times per week; 7 weeks; s.c.; 120 μg/mouse; twice per week; until sacrifice
Result:

Prevented NAFLD-induced CD4+ T-cell depletion in the liver and spleen, confirmed by IHC.
Shifted hepatic and splenic CD4+/CD8+ T cells toward a predominant CD4+>CD8+ pattern.
Did not significantly affect the hepatic or splenic M1>M2 macrophage, NKT>NK, or predominant Te CD4+/CD8+ patterns.
Increased splenic MDSC percentage but not hepatic MDSC.
Hepatic CD4+ T-cell subsets shifted from Th1>Th2=Th17=Treg to Th1>Th2=Treg>Th17; splenic CD4+ T-cell subsets shifted from Th1=Treg>Th2=Th17 to Th1=Th2=Treg>Th17.
No serum cytokines/chemokines were significantly modulated after 48 weeks of WD.
5/6 animals were tumor-bearing and 1/6 were tumor-free.
Did not affect body weight or liver steatosis.

Related Protocols :

Chemical Information

CAS No. 2640117-95-7
Molecular Weight 2106.51
Formula C₁₀₂H₁₆₀N₂₄O₂₄
SMILES

O=C(N[C@@H](C(C)C)C(N[C@@H](CCCCN)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H](CC(N)=O)C(N[C@@H](CCCCN)C(N2[C@@H](CCC2)C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H](C(C)C)C(N[C@@H](CC4=CC=CC=C4)C(N[C@@H](CC(C)C)C(N[C@@H](CCCC)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC(N)=O)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCCCN)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)C
Sequence

Ac-Val-Lys-Phe-Asn-Lys-Pro-Phe-Val-Phe-Leu-Nle-Ile-Glu-Gln-Asn-Thr-Lys-NH2
Sequence Shortening

Ac-VKFNKPFVFL-Nle-IEQNTK-NH2
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

Handling Instructions (2659 KB)

References

[1]. Toldo S, et al. Low-Density Lipoprotein Receptor-Related Protein-1 Is a Therapeutic Target in Acute Myocardial Infarction. JACC Basic Transl Sci. 2017 Oct 30;2(5):561-574.

[2]. Wang Z, et al. α1-Antitrypsin derived SP16 peptide demonstrates efficacy in rodent models of acute and neuropathic pain. FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 2022 Jan;36(1):e22093.

[3]. Soler Y, et al. SERPIN-Derived Small Peptide (SP16) as a Potential Therapeutic Agent against HIV-Induced Inflammatory Molecules and Viral Replication in Cells of the Central Nervous System. Cells. 2023 Feb 15;12(4):632.

[4]. Isbell M, et al. Restoration of CD4 T Cells during NAFLD without Modulation of the Hepatic Immunological Pattern Is Not Sufficient to Prevent HCC. Cancers. 2022 Nov 09;14(22):5502.

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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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SP16 peptide

All Akt Isoforms

All ERK Isoforms

All Toll-like Receptor (TLR) Isoforms

All NF-κB Isoforms

All Caspase Isoforms

All NOD-like Receptor (NLR) Isoforms

All Interleukin Related Isoforms

All HIV Isoforms