B7-33 (Relaxin)

Relaxin-2 Analog | Anti-Fibrotic & Cardiovascular

Weight: ~4,000 Da
Half-life: Not well characterized
5 studies
2020 latest
Emerging
Dose 100-250mcg
Frequency Once daily
Cycle 4-8 weeks (preclinical extrapolation)
Storage Lyophilized: freezer long-term. Reconstituted: 2-8 C for up to 28 days

Community Research

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B7-33 is a single-chain peptide analog of human relaxin-2 that selectively activates the relaxin family peptide receptor 1 (RXFP1). Unlike native relaxin-2, which requires a complex two-chain A/B structure connected by disulfide bonds, B7-33 achieves RXFP1 activation with a much simpler single-chain design. This makes it significantly easier and more cost-effective to synthesize. Preclinical research demonstrates potent anti-fibrotic, vasodilatory, and cardioprotective properties, positioning B7-33 as a promising therapeutic candidate for fibrotic diseases, heart failure, and vascular dysfunction.

Mechanism of Action

Selectively activates RXFP1, the primary receptor for relaxin-2, triggering downstream signaling cascades that inhibit fibroblast activation and collagen deposition, promote extracellular matrix remodeling via increased matrix metalloproteinase (MMP) activity, enhance nitric oxide-mediated vasodilation, and reduce inflammatory cytokine expression. B7-33 appears to preferentially engage pERK1/2 signaling pathways while showing reduced cAMP activation compared to native relaxin-2, suggesting biased agonism at RXFP1.

01 Potent anti-fibrotic activity across multiple organ systems
02 Improved vasodilation and vascular compliance
03 Cardioprotective effects and potential to attenuate cardiac remodeling
04 Much simpler to synthesize than native two-chain relaxin-2
05 Selective RXFP1 agonism with biased signaling profile
06 Preclinical efficacy in models of heart failure and fibrosis

Molecular Data

Molecular Weight
~4,000 Da
Type
Single-chain peptide
Amino Acid Sequence
Single-chain analog of relaxin-2 B-chain

Complex or non-standard sequence format

Research Indications

Cardiovascular
Cardiac Fibrosis effective

Reduces myocardial fibrosis and collagen deposition, attenuating adverse cardiac remodeling in preclinical heart failure models.

Vasodilation effective

Enhances nitric oxide-mediated vasodilation, reducing vascular resistance and improving blood flow in preclinical studies.

Heart Failure moderate

Demonstrates cardioprotective effects in animal models of heart failure, improving cardiac function and reducing fibrotic burden.

Anti-Fibrotic
Organ Fibrosis effective

Inhibits fibroblast differentiation into myofibroblasts and reduces extracellular matrix deposition in multiple organ systems.

Renal Fibrosis moderate

Shows protective effects against kidney fibrosis progression in preclinical disease models.

Dosing Protocols

Subcutaneous injection is the primary route studied in preclinical research. Dosing protocols are based on animal model data and have not been validated in human trials.

GoalDoseFrequencyRoute
Anti-fibrotic / Cardiovascular support100-250 mcg1x dailySubQ

Reconstitution Instructions

Materials Needed:
  • Bacteriostatic water (BAC)
  • Insulin syringes (0.5-1 mL)
  • Alcohol swabs
  • Peptide vial
  • Sterile work surface
  1. 1 Clean work area and hands thoroughly
  2. 2 Calculate required BAC water volume using calculator
  3. 3 Draw BAC water into syringe
  4. 4 Inject slowly down vial side (not directly onto powder)
  5. 5 Gently swirl until dissolved (never shake)
  6. 6 Store in refrigerator, use within 28 days

Interactions

++
Telmisartan
Potential synergistic effects for cardiac protection; both target complementary pathways involved in cardiac remodeling and fibrosis.
synergistic
+
BPC-157
No known negative interactions; different mechanisms of action with complementary tissue-repair and anti-fibrotic properties.
compatible

What to Expect

Week 1-2
Onset of vasodilatory effects; initial anti-fibrotic signaling activation
Week 2-4
Progressive reduction in fibrotic markers based on preclinical timelines
Week 4-8
Measurable improvements in tissue fibrosis and cardiovascular parameters in animal models

Side Effects & Safety

Common Side Effects

  • Injection site reactions (redness, mild irritation)
  • Potential transient hypotension due to vasodilatory effects

Stop Signs - Discontinue if:

  • Persistent or symptomatic hypotension (dizziness, lightheadedness, fainting)
  • Severe injection site reactions or signs of infection
  • Allergic reactions (rash, swelling, difficulty breathing)

Contraindications

  • Pre-existing hypotension or conditions exacerbated by vasodilation
  • Pregnancy or breastfeeding (no safety data available)
  • Concurrent use of potent antihypertensive agents without medical supervision
  • No human safety data exists -- all protocols are extrapolated from preclinical research

Quality Checklist

Good Signs

  • White to off-white lyophilized powder
  • Clear solution after reconstitution with no particles
  • Intact vacuum seal on vial

Warning Signs

  • Slight clumping that dissolves with gentle swirling (may occur from shipping)

Bad Signs

  • Discolored or wet powder indicating degradation
  • Cloudy solution, visible particles, or precipitates after reconstitution
  • Broken or missing vacuum seal

References

  • A single-chain peptide derived from the relaxin B-chain selectively activates RXFP1
    Hossain, M.A., et al.
    Chemical Science (2016)

    Identified B7-33 as a single-chain relaxin analog that selectively activates RXFP1, demonstrating that a simplified single-chain peptide can replicate key signaling functions of native two-chain relaxin-2.

  • The single-chain relaxin mimetic, B7-33, maintains anti-fibrotic activity in liver and kidney fibrosis models
    Hossain, M.A., et al.
    British Journal of Pharmacology (2020)

    B7-33 reduced fibrosis markers in both liver and kidney fibrosis models, demonstrating organ-protective anti-fibrotic effects comparable to native relaxin-2 despite its simplified structure.

  • The relaxin receptor as a therapeutic target -- perspectives from evolution and drug targeting
    Bathgate, R.A.D., et al.
    Pharmacology & Therapeutics (2018)

    Comprehensive review of RXFP1 as a drug target, discussing relaxin-2 and analogs including B7-33 for cardiovascular, fibrotic, and reproductive indications.

  • B7-33 replicates the vasoprotective effects of relaxin in mouse models of cardiovascular disease
    Marshall, S.A., et al.
    Annals of the New York Academy of Sciences (2017)

    B7-33 replicated the vasoprotective and anti-fibrotic effects of native relaxin in mouse models, reducing vascular stiffness and improving cardiovascular outcomes.

  • The role of relaxin and its receptor (RXFP1) in the pathogenesis and treatment of fibrotic diseases
    Samuel, C.S., et al.
    Molecular and Cellular Endocrinology (2017)

    Reviews the anti-fibrotic mechanisms of relaxin/RXFP1 signaling, including inhibition of TGF-beta-driven fibroblast activation and collagen synthesis, with implications for simplified analogs like B7-33.

Disclaimer

This information is for educational and research purposes only. Consult a healthcare professional before use.